DGIdb - HRH1 Gene Record

HRH1 3269 Druggable Genome

Alternate Names:

3269
HISTAMINE RECEPTOR H1
HRH1
H1-R
H1R
HH1R
hisH1
600167
5182
ENSG00000196639
OTTHUMG00000129719
P35367
HISTAMINE H1 RECEPTOR
HRH1_HUMAN
262
H<sub>1</sub> receptor
NM_000861
NP_000852
HISTAMINE H1 RECEPTOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P35367]
TTDS00086
HISTAMINE RECEPTOR 1
H1 HISTAMINE RECEPTOR
BE0000442
PA29456
T77913

Gene Info:

Interpro Acc	IPR000276
Uniprot Status	Swiss-Prot
Uniprot Evidence	1: Evidence at protein level
Interpro Short Name	7TM_GPCR_Rhodpsn
Human Readable Name	DRUGGABLE GENOME
Interpro Name	GPCR, rhodopsin-like, 7TM
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Interpro Type	Family
GuideToPharmacology Gene Category Name	Histamine receptors
GuideToPharmacology Gene Category ID	33
GuideToPharmacology Gene Type	gpcr
Transmembrane Helix Count	7
Target Subclass	Rhodopsin
Target Subclass	GPCR
Target Main Class	Receptors
Target Class	Receptors
Gene Biotype	PROTEIN_CODING

(11 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Karadağ et al., 1996, The role of histamine H1-receptors in the anticonvulsive effect of morphine against maximal electroconvulsive shock in mice., Jpn. J. Pharmacol.
Leurs et al., 1989, High affinity, saturable [3H]mepyramine binding sites on rat liver plasma membrane do not represent histamine H1-receptors. A warning., Biochem. Pharmacol.
Nosal et al., 2009, H1-antihistamines and oxidative burst of professional phagocytes., Neuro Endocrinol. Lett.
Gepdiremen et al., Contribution of the histaminergic receptor subtypes to histamine-induced cerebellar granular neurotoxicity., Pol J Pharmacol
Yanni et al., 1994, Preclinical efficacy of emedastine, a potent, selective histamine H1 antagonist for topical ocular use., J Ocul Pharmacol
Nath et al., 2001, Role of central histaminergic system in lorazepam withdrawal syndrome in rats., Pharmacol. Biochem. Behav.
Tsujii et al., 2007, Effects of sedative and non-sedative H1 antagonists on cognitive tasks: behavioral and near-infrared spectroscopy (NIRS) examinations., Psychopharmacology (Berl.)
Walther et al., 1990, New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine., Arzneimittelforschung
Miller et al., 1989, Factors in snake venoms that increase capillary permeability., J. Pharm. Pharmacol.
Claro et al., 1986, Phosphoinositide hydrolysis mediated by histamine H1-receptors in rat brain cortex., Eur. J. Pharmacol.
Suzuki et al., 2003, Histamine H1-receptor antagonists, promethazine and homochlorcyclizine, increase the steady-state plasma concentrations of haloperidol and reduced haloperidol., Ther Drug Monit
Smith et al., 1993, Histamine enhances the depolarizing afterpotential of immunohistochemically identified vasopressin neurons in the rat supraoptic nucleus via H1-receptor activation., Neuroscience
Paton et al., Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines)., Clin Pharmacokinet
Ikeda et al., 1997, Histamine-induced calcium released from cultured human mucosal microvascular endothelial cells from nasal inferior turbinate., Acta Otolaryngol.
Vasudevan SR et al., 2012, Shape-based reprofiling of FDA-approved drugs for the H₁ histamine receptor., J Med Chem
Christophe et al., 2003, Histamine H1 receptor antagonism by cetirizine in isolated guinea pig tissues: influence of receptor reserve and dissociation kinetics., Eur. J. Pharmacol.
Tamura et al., 2005, Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice., Pharmacology
Tashiro et al., 2004, Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography., J Clin Pharmacol
Tillement et al., 2003, Compared pharmacological characteristics in humans of racemic cetirizine and levocetirizine, two histamine H1-receptor antagonists., Biochem. Pharmacol.
Cavero et al., 1999, Preclinical in vitro cardiac electrophysiology: a method of predicting arrhythmogenic potential of antihistamines in humans?, Drug Saf
Zhang L et al., 2013, The clinical use of cetirizine in the treatment of allergic rhinitis., Pharmacology
Portnoy JM et al., 2004, Review of cetirizine hydrochloride for the treatment of allergic disorders., Expert Opin Pharmacother
Ito et al., 1996, Role of tachykinin and bradykinin receptors and mast cells in gaseous formaldehyde-induced airway microvascular leakage in rats., Eur. J. Pharmacol.
Yokoyama et al., 1993, Proconvulsant effect of ketotifen, a histamine H1 antagonist, confirmed by the use of d-chlorpheniramine with monitoring electroencephalography., Methods Find Exp Clin Pharmacol
Mita et al., 1995, Comparison of anti-allergic activities of the histamine H1 receptor antagonists epinastine, ketotifen and oxatomide in human leukocytes., Arzneimittelforschung
Hashimoto et al., 2006, Lysophosphatidic acid (LPA) induces plasma exudation and histamine release in mice via LPA receptors., J. Pharmacol. Sci.
Okabe et al., 1992, Effect of ketotifen on acute gastric lesions and gastric secretion in rats., Jpn. J. Pharmacol.
Werner-Klein et al., 2008, Development and characterisation of a novel and rapid lung eosinophil influx model in the rat., Pulm Pharmacol Ther
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
Yasuda et al., 1999, Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes., Pharmacotherapy
Onaran et al., 1990, Kinetics of antagonism at histamine-H1 receptors in isolated rabbit arteries., Naunyn Schmiedebergs Arch. Pharmacol.
Bökesoy et al., 1991, Atypical Schild plots with histamine H1 receptor agonists and antagonists in the rabbit aorta., Eur. J. Pharmacol.
KRAKOWSKI, 1962, Propiomazine for control of insomnia in nervous disorders., Am J Psychiatry
Kim DH et al., 2009, Building a better antipsychotic: receptor targets for the treatment of multiple symptom dimensions of schizophrenia., Neurotherapeutics
Ishikawa et al., 2007, Influences of histamine H1 receptor antagonists on maximal electroshock seizure in infant rats., Biol. Pharm. Bull.
Piao et al., 2007, Potentiation by neuropeptide Y of histamine H1 receptor-mediated contraction in rat blood vessels., Vascul. Pharmacol.
Wang et al., 2007, Self-administration of cocaine-antihistamine combinations: super-additive reinforcing effects., Eur. J. Pharmacol.
Hasala et al., First-generation antihistamines diphenhydramine and chlorpheniramine reverse cytokine-afforded eosinophil survival by enhancing apoptosis., Allergy Asthma Proc
Havas et al., 1986, The effects of combined H1 and H2 histamine antagonists on alterations in nasal airflow resistance induced by topical histamine provocation., J. Allergy Clin. Immunol.
Kesiova et al., Effects of diphenhydramine and famotidine on lipid peroxidation and activities of antioxidant enzymes in different rat tissues., Pharmacol Rep
Sawynok et al., 1999, Peripheral antinociceptive actions of desipramine and fluoxetine in an inflammatory and neuropathic pain test in the rat., Pain
Dorsch et al., 1984, Sequential histamine inhalations cause increased bronchial histamine reactivity in guinea pigs: role of platelets, thromboxanes and prostacyclin., Naunyn Schmiedebergs Arch. Pharmacol.
Schran et al., 1996, The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations., J Clin Pharmacol
Taniguchi et al., 1991, Inhibitory effects of histamine H1 receptor blocking drugs on metabolic activations of neutrophils., J. Pharmacobio-dyn.
Taniguchi et al., 1987, [Effects of antiallergic agents on polymorphonuclear leukocytes. The inhibition of arachidonic acid release and superoxide production]., Nippon Yakurigaku Zasshi
Oishi et al., 1994, Comparison of the effects of eleven histamine H1-receptor antagonists on monoamine turnover in the mouse brain., Naunyn Schmiedebergs Arch. Pharmacol.
Hallberg et al., 1984, Demonstration of histamine receptors on human platelets by flow cytometry., Scand J Haematol
Thomson et al., 1980, Effect of inhaled H1 and H2 receptor antagonist in normal and asthmatic subjects., Thorax
Hayashi et al., 1976, Atrial T (Ta) loop in dogs with or without atrial injury., Am. Heart J.
Thomas et al., 1985, The influence of ranitidine, alone and in combination with clemastine, on histamine-mediated cutaneous weal and flare reactions in human skin., Br J Clin Pharmacol
McCormack, 2015, Cariprazine: First Global Approval., Drugs
Chattopadhyay et al., 1998, Altered membrane permeability as the basis of bactericidal action of methdilazine., J. Antimicrob. Chemother.
Dasgupta et al., 2010, Experimental analyses of synergistic combinations of antibiotics with a recently recognised antibacterial agent, lacidipine., Eur. J. Clin. Microbiol. Infect. Dis.
Wiseman et al., 1996, Ebastine. a review of its pharmacological properties and clinical efficacy in the treatment of allergic disorders., Drugs
Wang et al., 2002, Ketoconazole potentiates terfenadine-induced apoptosis in human Hep G2 cells through inhibition of cytochrome p450 3A4 activity., J. Cell. Biochem.
Nicholson et al., 1983, The H1-antagonist mequitazine: studies on performance and visual function., Eur. J. Clin. Pharmacol.
ter Laak et al., 1995, The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor., J. Med. Chem.
Yakuo et al., 1994, [Pharmacological study of ebastine, a novel histamine H1-receptor antagonist]., Nippon Yakurigaku Zasshi
Nakamura et al., 1998, Oxidation of histamine H1 antagonist mequitazine is catalyzed by cytochrome P450 2D6 in human liver microsomes., J. Pharmacol. Exp. Ther.
Kurenova et al., 2009, Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo., J. Med. Chem.
McLeod et al., 1998, Antitussive action of antihistamines is independent of sedative and ventilation activity in the guinea pig., Pharmacology
Sadofsky et al., 2008, Transient receptor potential vanilloid-1-mediated calcium responses are inhibited by the alkylamine antihistamines dexbrompheniramine and chlorpheniramine., Exp. Lung Res.
de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem
Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.
Kano et al., 2004, Decreased histamine H1 receptor binding in the brain of depressed patients., Eur. J. Neurosci.
Figueiredo et al., 1990, Mechanism of action of doxepin in the treatment of chronic urticaria., Fundam Clin Pharmacol
Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr
Tran et al., 1981, [3H]doxepin interactions with histamine H1-receptors and other sites in guinea pig and rat brain homogenates., Eur. J. Pharmacol.
Singh et al., 2007, Novel therapeutic usage of low-dose doxepin hydrochloride., Expert Opin Investig Drugs
Leysen et al., 1994, Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity., J Clin Psychiatry
Roegge et al., 2007, Histamine H1 receptor involvement in prepulse inhibition and memory function: relevance for the antipsychotic actions of clozapine., Pharmacol. Biochem. Behav.
Haria et al., 1994, Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders., Drugs
Clissold et al., 1989, Loratadine. A preliminary review of its pharmacodynamic properties and therapeutic efficacy., Drugs
Singh et al., 1998, Causal prophylactic activity of antihistaminic agents against Plasmodium yoelii nigeriensis infection in Swiss mice., Acta Trop.
Mann et al., 1989, Nonsedating histamine H1-receptor antagonists., Clin Pharm
Witek et al., 1992, The effects of phenindamine tartrate on sleepiness and psychomotor performance., J. Allergy Clin. Immunol.
van Drooge et al., 1991, The histamine H1-receptor antagonist binding site. Part I: Active conformation of cyproheptadine., J. Comput. Aided Mol. Des.
Hals et al., 1988, Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites., Life Sci.
Han et al., 2006, Phospholipase Cbeta 3 mediates the scratching response activated by the histamine H1 receptor on C-fiber nociceptive neurons., Neuron
Spahr et al., 2007, Histamine H1 blocker hydroxyzine improves sleep in patients with cirrhosis and minimal hepatic encephalopathy: a randomized controlled pilot trial., Am. J. Gastroenterol.
Tanimoto et al., 2007, Histamine upregulates the expression of inducible nitric oxide synthase in human intimal smooth muscle cells via histamine H1 receptor and NF-kappaB signaling pathway., Arterioscler. Thromb. Vasc. Biol.
Miyoshi et al., 2006, Recent advances in molecular pharmacology of the histamine systems: regulation of histamine H1 receptor signaling by changing its expression level., J. Pharmacol. Sci.
Suzuki et al., 2007, A dual antagonist for chemokine CCR3 receptor and histamine H1 receptor., Eur. J. Pharmacol.
Lacour et al., 2001, Histamine and betahistine in the treatment of vertigo: elucidation of mechanisms of action., CNS Drugs
Barak, 2008, Betahistine: what's new on the agenda?, Expert Opin Investig Drugs
Jongejan A et al., 2005, Linking agonist binding to histamine H1 receptor activation., Nat Chem Biol
Parsons et al., 2006, Histamine and its receptors., Br. J. Pharmacol.
Moriyama et al., 2009, Receptor mediation and nociceptin inhibition of bradykinin-induced plasma extravasation in the knee joint of the rat., Inflamm. Res.
Chhabria et al., 2009, Design, synthesis and histamine H1-receptor antagonistic activity of some novel 4-amino-2-(substituted)-5-(substituted) aryl-6-[(substituted aryl) amino] pyrimidines., Arzneimittelforschung
Snowman et al., 1990, Cetirizine: actions on neurotransmitter receptors., J. Allergy Clin. Immunol.
Mojtahedin et al., Antinociception induced by central administration of histamine in the formalin test in rats., Indian J. Physiol. Pharmacol.
Taylor et al., 1986, Interactions of verapamil, D 600, flunarizine and nifedipine with cerebral histamine-receptors., Neurochem. Int.
Ohta et al., 1999, Role of endogenous serotonin and histamine in the pathogenesis of gastric mucosal lesions in unanaesthetised rats with a single treatment of compound 48/80, a mast cell degranulator., Pharmacol. Res.
Sansone, Antihistaminic-opioid combination: effect on locomotor activity in mice., Pol J Pharmacol Pharm
Shimizu et al., 1982, [Drug sensitivity of the isolated stomach and ileal preparation from a vole]., Nihon Heikatsukin Gakkai Zasshi
Chiba, 1976, Blocking effect of tripelennamine on histamine--induced positive chronotropic and inotropic responses of the dog atrium., Tohoku J. Exp. Med.
Suzuki et al., 1997, Interactions between H1-antagonists and opioids: a drug discrimination study., Psychopharmacology (Berl.)
Mercier et al., 1974, Electro-encephalographic study on the action of the combination meprobamate-aceprometazine on various cerebral systems., Arzneimittelforschung
Li J et al., 2020, Human H1 receptor (HRH1) gene polymorphism is associated with the severity of side effects after desloratadine treatment in Chinese patients with chronic spontaneous uticaria., Pharmacogenomics J
Simons et al., 2003, Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis., J. Allergy Clin. Immunol.
Cieślewicz et al., 1995, [Effect of loratadine, selective antagonist of histamine H1 receptors, on histamine-induced bronchoconstriction]., Pneumonol Alergol Pol
Devillier et al., 2008, Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review., Clin Pharmacokinet
Letari et al., 1994, Effects of loratadine on cytosolic Ca2+ levels and leukotriene release: novel mechanisms of action independent of the anti-histamine activity., Eur. J. Pharmacol.
Wu et al., 2004, Desloratadine inhibits constitutive and histamine-stimulated nuclear factor-kappaB activity consistent with inverse agonism at the histamine H1 Receptor., Int. Arch. Allergy Immunol.
Dhanya et al., Comparative efficacy of levocetirizine, desloratidine and fexofenadine by histamine wheal suppression test., Indian J Dermatol Venereol Leprol
DuBuske, 2007, Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy., Am J Clin Dermatol
Abbas et al., 2004, A novel membrane sensor for histamine H1-receptor antagonist "fexofenadine"., Anal Sci
Grzelewska-Rzymowska et al., 2003, [Effect of fexofenadine--selective antagonist of histamine receptor (H1) on histamine-induced bronchoconstriction]., Pol. Merkur. Lekarski
Markham et al., 1998, Fexofenadine., Drugs
Smith et al., 2009, Fexofenadine: biochemical, pharmacokinetic and pharmacodynamic properties and its unique role in allergic disorders., Expert Opin Drug Metab Toxicol
Amon et al., 2000, In vitro studies with fexofenadine, a new nonsedating histamine H1 receptor antagonist, on isolated human basophils., Inflamm. Res.
Ziganshina et al., 1996, Acute paw oedema formation induced by ATP: re-evaluation of the mechanisms involved., Inflamm. Res.
Estelle et al., 1999, H1-receptor antagonists: safety issues., Ann. Allergy Asthma Immunol.
Kuzmin et al., 1999, The effect of histamine receptor antagonists on stress-induced catecholamine secretion: an adrenomedullary microdialysis study in the rat., Eur. J. Pharmacol.
Simons, 1994, H1-receptor antagonists. Comparative tolerability and safety., Drug Saf
Peroutka et al., 1981, Two distinct serotonin receptors: regional variations in receptor binding in mammalian brain., Brain Res.
Hiroi et al., 1995, Mepyramine, a histamine H1 receptor antagonist, inhibits the metabolic activity of rat and human P450 2D forms., J. Pharmacol. Exp. Ther.
Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.
Keks et al., 1999, Risperidone (Risperdal): clinical experience with a new antipsychosis drug., Expert Opin Investig Drugs
Schreiber et al., 1997, Augmentation of opioid induced antinociception by the atypical antipsychotic drug risperidone in mice., Neurosci. Lett.
Corena-McLeod M, 2015, Comparative Pharmacology of Risperidone and Paliperidone., Drugs R D
Sugimoto et al., 1999, Effects of levocabastine on lipid mediator release from guinea pig lung fragments., Acta Med. Okayama
Chalon et al., 1996, Molecular cloning of a levocabastine-sensitive neurotensin binding site., FEBS Lett.
Betancur et al., 1998, Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain., Eur. J. Pharmacol.
Akiyoshi et al., 2002, [Pharmacological and clinical properties of levocabastine hydrochloride (eye drop and nasal spray), a selective H1 antagonist]., Nippon Yakurigaku Zasshi
Yamada et al., 1998, Distinct functional characteristics of levocabastine sensitive rat neurotensin NT2 receptor expressed in Chinese hamster ovary cells., Life Sci.
Santos et al., 1995, Blockers for excitatory effects of achatin-I, a tetrapeptide having a D-phenylalanine residue, on a snail neurone., Eur. J. Pharmacol.
Maurer et al., 1988, Identification and differentiation of alkylamine antihistamines and their metabolites in urine by computerized gas chromatography-mass spectrometry., J. Chromatogr.
Wood-Baker et al., 1995, A double-blind, placebo controlled study of the effect of the specific histamine H1-receptor antagonist, terfenadine, in chronic severe asthma., Br J Clin Pharmacol
Salata et al., 1995, Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine., Circ. Res.
Rafferty et al., 1987, Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways., Am. Rev. Respir. Dis.
Kishimoto et al., 1997, Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine., Res. Commun. Mol. Pathol. Pharmacol.
Phillips et al., 1989, The effect of histamine-H1 receptor antagonism with terfenadine on concentration-related AMP-induced bronchoconstriction in asthma., Clin. Exp. Allergy
Leza et al., 1990, H1- and H2-histamine receptor blockers and opiate analgesia in mice., Methods Find Exp Clin Pharmacol
Noguchi et al., 1992, The suppression of olfactory bulbectomy-induced muricide by antidepressants and antihistamines via histamine H1 receptor blocking., Physiol. Behav.
Ramadan et al., 2006, Spectrophotometric determination of carbinoxamine maleate in pharmaceutical formulations by ternary complex formation with Cu(II) and eosin., Anal. Biochem.
Darby, 1975, Nutrition, food needs and technologic priorities: the World Food Conference., Nutr. Rev.
Yang et al., 2009, [1,2]-Anionic rearrangement of 2-benzyloxypyridine and related pyridyl ethers., J. Org. Chem.
Sakaguchi et al., 2008, Hydroxyzine, a first generation H(1)-receptor antagonist, inhibits human ether-a-go-go-related gene (HERG) current and causes syncope in a patient with the HERG mutation., J. Pharmacol. Sci.
Chen, 2008, Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine., Curr. Med. Chem.
Altamura AC et al., 2013, Understanding the pharmacokinetics of anxiolytic drugs., Expert Opin Drug Metab Toxicol
Halpert et al., 2002, Mechanisms and abuse liability of the anti-histamine dimenhydrinate., Neurosci Biobehav Rev
Martins et al., 1992, Interference of cetirizine with the late eosinophil accumulation induced by either PAF or compound 48/80., Br. J. Pharmacol.
Pasquale et al., 1992, Suppression by cetirizine of pleurisy triggered by antigen in actively sensitized rats., Eur. J. Pharmacol.
Nowak et al., 1983, Interaction between mianserin, an antidepressant drug, and central H1- and H2-histamine-receptors: in vitro and in vivo studies and radioreceptor assay., Neuropharmacology
Grinshpoon et al., 2000, Beneficial effect of the addition of the 5-HT 2A/2C and alpha2 antagonist mianserin to ongoing haloperidol treatment in drug-resistant chronically hospitalized schizophrenic patients., Eur. Psychiatry
Csaba et al., 2003, Prolonged effect of the tricyclic antidepressant, mianserin on the serotonin and histamine content of young rats' white blood cells and mast cells. A case of late-imprinting., Pharmacol. Res.
Simons et al., 2011, Histamine and H1-antihistamines: celebrating a century of progress., J. Allergy Clin. Immunol.
Altschuler et al., 2005, Using histamine (H1) antagonists, in particular atypical antipsychotics, to treat anemia of chronic disease via interleukin-6 suppression., Med. Hypotheses
Poyurovsky et al., 2005, The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients., Int Clin Psychopharmacol
Uchida et al., 2007, Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine., Life Sci.
Bymaster et al., 1999, Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro., Schizophr. Res.
Rasmussen et al., 2005, Preclinical pharmacology of FMPD [6-fluoro-10-[3-(2-methoxyethyl)-4-methyl-piperazin-1-yl]-2-methyl-4H-3-thia-4,9-diaza-benzo[f]azulene]: a potential novel antipsychotic with lower histamine H1 receptor affinity than olanzapine., J. Pharmacol. Exp. Ther.
Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
Baroody et al., 2000, Antiallergic effects of H1-receptor antagonists., Allergy
Cieślewicz et al., 1992, [Effect of loratadine--selective antagonist of histamine (H1) receptor--on allergen-induced bronchoconstriction in atopic asthmatics]., Pneumonol Alergol Pol
Menardo et al., A review of loratadine in the treatment of patients with allergic bronchial asthma., Clin Ther
Howarth, 1990, Histamine and asthma: an appraisal based on specific H1-receptor antagonism., Clin. Exp. Allergy
Grzelewska-Rzymowska et al., 1992, [Effect of loratadine (LO), a selective H1 antagonist, on histamine-induced bronchoconstriction]., Pneumonol Alergol Pol
Arnt, 1995, Differential effects of classical and newer antipsychotics on the hypermotility induced by two dose levels of D-amphetamine., Eur. J. Pharmacol.
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
Howarth et al., 1984, Astemizole, a potent histamine H1-receptor antagonist: effect in allergic rhinoconjunctivitis, on antigen and histamine induced skin weal responses and relationship to serum levels., Br J Clin Pharmacol
Krstenansky et al., 1987, Astemizole: a long-acting, nonsedating antihistamine., Drug Intell Clin Pharm
Llenas et al., 1999, Cardiotoxicity of histamine and the possible role of histamine in the arrhythmogenesis produced by certain antihistamines., Drug Saf
Kaliner et al., Non-sedating antihistamines., Allergy Proc
Richards et al., 1984, Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy., Drugs
Swiader et al., Effect of histamine receptor antagonists on aminophylline-induced seizures and lethality in mice., Pharmacol Rep
Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
Citrome, 2011, Role of sublingual asenapine in treatment of schizophrenia., Neuropsychiatr Dis Treat
Nicholson et al., 1991, Sedation and histamine H1-receptor antagonism: studies in man with the enantiomers of chlorpheniramine and dimethindene., Br. J. Pharmacol.
Hasenöhrl et al., 2001, Comparison of intra-accumbens injection of histamine with histamine H1-receptor antagonist chlorpheniramine in effects on reinforcement and memory parameters., Behav. Brain Res.
Yasuda et al., 1995, Chlorpheniramine plasma concentration and histamine H1-receptor occupancy., Clin. Pharmacol. Ther.
Tagawa et al., 2001, Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-chlorpheniramine, a classical antihistamine., Br J Clin Pharmacol
Kanba et al., 1984, Histamine H1 receptors in human brain labelled with [3H]doxepin., Brain Res.
Cavero et al., 1981, Effects of mianserin, desipramine and maprotiline on blood pressure responses evoked by acetylcholine, histamine and 5-hydroxytryptamine in rats., Br. J. Pharmacol.
Palmer et al., 1978, Histamine-, norepinephrine-, and dopamine-sensitive central adenylate cyclases: effects of chlorpromazine derivatives and butaclamol., Arch Int Pharmacodyn Ther
Church et al., 1983, The characteristics of inhibition of histamine release from human lung fragments by sodium cromoglycate, salbutamol and chlorpromazine., Br. J. Pharmacol.
Ruffolo et al., 1978, Kinetics of blockade of different receptors by chlorpromazine in rabbit stomach strips., Eur. J. Pharmacol.
Johnson et al., 1979, Inhibition of histamine release and ionophore-induced calcium flux in rat mast cells by lidocaine and chlorpromazine., Agents Actions
Golden et al., 1999, Efficacy and safety of azelastine nasal spray for the treatment of allergic rhinitis., J Am Osteopath Assoc
Casale, 1989, The interaction of azelastine with human lung histamine H1, beta, and muscarinic receptor-binding sites., J. Allergy Clin. Immunol.
Antépara et al., [Investigation of the efficacy and tolerability of azelastine nasal spray versus ebastine tablets in patients with seasonal allergic rhinitis]., Allergol Immunopathol (Madr)
Conde Hernández et al., 1995, Comparison of azelastine nasal spray and oral ebastine in treating seasonal allergic rhinitis., Curr Med Res Opin
Bernstein, 2007, Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability., Curr Med Res Opin
Horak, 2008, Effectiveness of twice daily azelastine nasal spray in patients with seasonal allergic rhinitis., Ther Clin Risk Manag
Procopiou et al., 2011, The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis., J. Med. Chem.
Murota et al., 2008, Emedastine difumarate inhibits histamine-induced collagen synthesis in dermal fibroblasts., J Investig Allergol Clin Immunol
Corrado et al., 2004, Clinical study of the therapeutic efficacy and safety of emedastine difumarate versus terfenadine in the treatment of seasonal allergic rhinitis., Arzneimittelforschung
Sharif et al., 1994, Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies., J Ocul Pharmacol
Inagaki et al., 1998, Characterization of antihistamines using biphasic cutaneous reaction in BALB/c mice., Life Sci.
Murota et al., 2009, Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases., Expert Opin Pharmacother
Ding P et al., 2017, PTS: a pharmaceutical target seeker., Database (Oxford)
Lapa et al., 2005, Diphenylpyraline, a histamine H1 receptor antagonist, has psychostimulant properties., Eur. J. Pharmacol.
Nakai et al., 1991, Decreased histamine H1 receptors in the frontal cortex of brains from patients with chronic schizophrenia., Biol. Psychiatry
Weis et al., 2008, Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives., Bioorg. Med. Chem.
Enright et al., 2010, Effects of the histamine H1 antagonist chlorcyclizine on rat fetal palate development., Birth Defects Res. B Dev. Reprod. Toxicol.
Merlos M et al., 1997, Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF)., J Pharmacol Exp Ther
Andoh et al., 2006, Suppression by bepotastine besilate of substance P-induced itch-associated responses through the inhibition of the leukotriene B4 action in mice., Eur. J. Pharmacol.
Ivgy-May et al., 2015, Esmirtazapine in non-elderly adult patients with primary insomnia: efficacy and safety from a randomized, 6-week sleep laboratory trial., Sleep Med.
Ohmori et al., 2004, Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug., Arzneimittelforschung
Kaliner et al., Comprehensive review of olopatadine: the molecule and its clinical entities., Allergy Asthma Proc
Ohmori et al., 2001, [Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride' (olopatadine), an antiallergic drug]., Nippon Yakurigaku Zasshi
Roland et al., 2010, Olopatadine nasal spray for the treatment of seasonal allergic rhinitis in patients aged 6 years and older., Expert Opin Pharmacother
Ohmori et al., 2002, Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug., Jpn. J. Pharmacol.
Roland et al., 2010, Olopatadine nasal spray for the treatment of allergic rhinitis., Expert Rev Clin Immunol
Yanni et al., 1996, The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent., J Ocul Pharmacol Ther
Rumore et al., 1985, Analgesic effects of antihistaminics., Life Sci.
Sadava et al., 1984, Tricyclic antidepressant drugs affect histamine receptors in human leukocytes., Life Sci.
Taylor JE et al., 1980, High affinity binding of tricyclic antidepressants to histamine H1-receptors: fact and artifact., Eur J Pharmacol
Bobo, 2013, Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults., Expert Rev Clin Pharmacol
Brandes et al., 1987, Histamine and growth: interaction of antiestrogen binding site ligands with a novel histamine site that may be associated with calcium channels., Cancer Res.
Moree et al., 2010, Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia., Bioorg. Med. Chem. Lett.
Pfaff et al., 1995, The (S)-(+)-enantiomer of dimethindene: a novel M2-selective muscarinic receptor antagonist., Eur. J. Pharmacol.
Niemegeers, 1982, Antiemetic specificity of dopamine antagonists., Psychopharmacology (Berl.)
Kachur JF et al., 1988, Antihistaminic and antimuscarinic effects of amitriptyline on guinea pig ileal electrolyte transport and muscle contractility in vitro., J Pharmacol Exp Ther
Richelson E, 1979, Tricyclic antidepressants and histamine H1 receptors., Mayo Clin Proc
Moreau et al., 1995, Phototoxic and photoprotective effects of topical isothipendyl., Photodermatol Photoimmunol Photomed
Ferrer, 2011, Pharmacokinetic evaluation of levocetirizine., Expert Opin Drug Metab Toxicol
Berger et al., 1996, Trimipramine: a challenge to current concepts on antidepressives., Eur Arch Psychiatry Clin Neurosci
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Wander et al., 1986, Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro., Eur. J. Pharmacol.
Scatton et al., 2001, The preclinical pharmacologic profile of tiapride., Eur. Psychiatry
Wang et al., 2016, Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine., Ther Clin Risk Manag
Vande Griend JP et al., 2012, Histamine-1 receptor antagonism for treatment of insomnia., J Am Pharm Assoc (2003)
Salvi V et al., 2016, H1-histamine receptor affinity predicts weight gain with antidepressants., Eur Neuropsychopharmacol
Sato H et al., 2013, Histamine H₁ receptor occupancy by the new-generation antidepressants fluvoxamine and mirtazapine: a positron emission tomography study in healthy volunteers., Psychopharmacology (Berl)
Gillman, 2007, Tricyclic antidepressant pharmacology and therapeutic drug interactions updated., Br. J. Pharmacol.
Kulkarni et al., 2006, Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors., Bioorg. Med. Chem.
de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
Megens et al., 1994, Survey on the pharmacodynamics of the new antipsychotic risperidone., Psychopharmacology (Berl.)
Cohen, Risperidone., Pharmacotherapy
Gilday E et al., 2012, Clinical pharmacology of paliperidone palmitate a parenteral long-acting formulation for the treatment of schizophrenia., Rev Recent Clin Trials
Cicek E et al., 2017, Bilateral Pretibial Edema Associated with Paliperidone Palmitate Long-acting Injectable: A Case Report., Clin Psychopharmacol Neurosci
Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
Isah AO et al., 1991, Clinical pharmacology of prochlorperazine in healthy young males., Br J Clin Pharmacol
Fabre et al., [Mechanisms of action of antidepressants: new data from Escitalopram]., Encephale
Bareggi et al., 2007, The use of escitalopram beyond major depression: pharmacological aspects, efficacy and tolerability in anxiety disorders., Expert Opin Drug Metab Toxicol
Sanchez C et al., 2014, A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike?, Int Clin Psychopharmacol
Roll et al., 1993, [Interaction of tolazoline and cimetidine in persistent fetal circulation of the newborn infant]., Monatsschr Kinderheilkd
Kishi T et al., 2013, Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials., CNS Drugs
Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
SCUDI JV et al., 1948, Pharmacologic characteristics of neohetramine, a new antihistaminic drug., J Allergy
AARON TH et al., 1948, Neohetramine and thephorin; two new antihistaminic drugs., Can Med Assoc J
Westenberg HG et al., 2006, Tolerability and safety of fluvoxamine and other antidepressants., Int J Clin Pract
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Vinod KY et al., 2002, Lamotrigine induced selective changes in 5-HT(1A) receptor mediated response in rat brain., Neurochem Int
Bourin M et al., 2005, Evidence for the activity of lamotrigine at 5-HT(1A) receptors in the mouse forced swimming test., J Psychiatry Neurosci
Abelaira HM et al., 2012, Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats., Pharmacol Biochem Behav
Jarema M et al., 2011, [Trazodon--the antidepressant: mechanism of action and its position in the treatment of depression]., Psychiatr Pol

EPINASTINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Antagonism of 5 nM [3H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Tsujii et al., 2007, Effects of sedative and non-sedative H1 antagonists on cognitive tasks: behavioral and near-infrared spectroscopy (NIRS) examinations., Psychopharmacology (Berl.)

Walther et al., 1990, New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine., Arzneimittelforschung

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

CYPROHEPTADINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

CYCLIZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Antagonist

Publications:

Leza et al., 1990, H1- and H2-histamine receptor blockers and opiate analgesia in mice., Methods Find Exp Clin Pharmacol

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

DIMENHYDRINATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:

Halpert et al., 2002, Mechanisms and abuse liability of the anti-histamine dimenhydrinate., Neurosci Biobehav Rev

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
ALCAFTADINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:

Simons et al., 2011, Histamine and H1-antihistamines: celebrating a century of progress., J. Allergy Clin. Immunol.

ASENAPINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Trial Name Asenapine

Publications:

Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)

Citrome, 2011, Role of sublingual asenapine in treatment of schizophrenia., Neuropsychiatr Dis Treat

RUPATADINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Merlos M et al., 1997, Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF)., J Pharmacol Exp Ther
DOTHIEPIN HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

Gillman, 2007, Tricyclic antidepressant pharmacology and therapeutic drug interactions updated., Br. J. Pharmacol.
TRIMEPRAZINE TARTRATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
HYDROXYZINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
CIPROXIFAN HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:
SERTINDOLE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
ACRIVASTINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
FEXOFENADINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:
LEVOCABASTINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
LY2624803 HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:
DIPHENHYDRAMINE CITRATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:
OLOPATADINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
A-349,821 HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inverse agonist

Publications:
CARBINOXAMINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
BEPOTASTINE BESYLATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
TRIPELENNAMINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:
DIPHENHYDRAMINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
ESMIRTAZAPINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
THIORIDAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
TOLAZOLINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor agonist

Direct Interaction yes

Publications:
TRIMIPRAMINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
PIPAMPERONE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
DOXYLAMINE SUCCINATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
ARPROMIDINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PITOLISANT HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:
AZELASTINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:
DEXBROMPHENIRAMINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
LEVOCETIRIZINE DIHYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
TRIFLUOPERAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
METHDILAZINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
DIPHENYLPYRALINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
CLOBENPROPIT HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
MOLINDONE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PYRILAMINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
TRIPROLIDINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
ORPHENADRINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
MK-0249 HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:
CYCLIZINE LACTATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
CETIRIZINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
FLUPHENAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
VAPITADINE DIHYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
PROMETHAZINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
TRIPELENNAMINE CITRATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
EPINASTINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
CLEMASTINE FUMARATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
CHLORPHENIRAMINE POLISTIREX HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
VILAZODONE HRH1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

Publications:
DEXCHLORPHENIRAMINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
chembl:CHEMBL351231 HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

Publications:
chembl:CHEMBL472273 HRH1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Publications:
KETOTIFEN FUMARATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
CYPROHEPTADINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
AZATADINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
CHLORPHENIRAMINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
MECLIZINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
EMEDASTINE DIFUMARATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
PERPHENAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PHENIRAMINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
IMPROMIDINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PROPIOMAZINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
chembl:CHEMBL361355 HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
HISTAMINE PHOSPHATE HRH1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor agonist

Direct Interaction yes

Publications:

MIZOLASTINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

BUCLIZINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
ORPHENADRINE CITRATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
CONESSINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:
ZOTEPINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
FLUSPIRILENE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
THIOTHIXENE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PIMOZIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
BROMODIPHENHYDRAMINE HYDROCHLORIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
HYDROXYZINE PAMOATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
BROMPHENIRAMINE MALEATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:
ANTAZOLINE PHOSPHATE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Publications:

BROMODIPHENHYDRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

PHENIRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

inverse agonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Karadağ et al., 1996, The role of histamine H1-receptors in the anticonvulsive effect of morphine against maximal electroconvulsive shock in mice., Jpn. J. Pharmacol.

Leurs et al., 1989, High affinity, saturable [3H]mepyramine binding sites on rat liver plasma membrane do not represent histamine H1-receptors. A warning., Biochem. Pharmacol.

Nosal et al., 2009, H1-antihistamines and oxidative burst of professional phagocytes., Neuro Endocrinol. Lett.

PROMETHAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Antagonist

Publications:

Miller et al., 1989, Factors in snake venoms that increase capillary permeability., J. Pharm. Pharmacol.

Claro et al., 1986, Phosphoinositide hydrolysis mediated by histamine H1-receptors in rat brain cortex., Eur. J. Pharmacol.

Suzuki et al., 2003, Histamine H1-receptor antagonists, promethazine and homochlorcyclizine, increase the steady-state plasma concentrations of haloperidol and reduced haloperidol., Ther Drug Monit

CETIRIZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name cetirizine HCl,Zyrtec

Novel drug target Established target

Direct Interaction? True

Publications:

Christophe et al., 2003, Histamine H1 receptor antagonism by cetirizine in isolated guinea pig tissues: influence of receptor reserve and dissociation kinetics., Eur. J. Pharmacol.

Tamura et al., 2005, Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice., Pharmacology

Tashiro et al., 2004, Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography., J Clin Pharmacol

KETOTIFEN HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name ketotifen fumarate,Zaditen, Zaditor

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

Ito et al., 1996, Role of tachykinin and bradykinin receptors and mast cells in gaseous formaldehyde-induced airway microvascular leakage in rats., Eur. J. Pharmacol.

Yokoyama et al., 1993, Proconvulsant effect of ketotifen, a histamine H1 antagonist, confirmed by the use of d-chlorpheniramine with monitoring electroencephalography., Methods Find Exp Clin Pharmacol

Mita et al., 1995, Comparison of anti-allergic activities of the histamine H1 receptor antagonists epinastine, ketotifen and oxatomide in human leukocytes., Arzneimittelforschung

BROMPHENIRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Yasuda et al., 1999, Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes., Pharmacotherapy

Onaran et al., 1990, Kinetics of antagonism at histamine-H1 receptors in isolated rabbit arteries., Naunyn Schmiedebergs Arch. Pharmacol.

PROPIOMAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

KRAKOWSKI, 1962, Propiomazine for control of insomnia in nervous disorders., Am J Psychiatry

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

DIPHENHYDRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Antagonist

Publications:

Ishikawa et al., 2007, Influences of histamine H1 receptor antagonists on maximal electroshock seizure in infant rats., Biol. Pharm. Bull.

Piao et al., 2007, Potentiation by neuropeptide Y of histamine H1 receptor-mediated contraction in rat blood vessels., Vascul. Pharmacol.

Wang et al., 2007, Self-administration of cocaine-antihistamine combinations: super-additive reinforcing effects., Eur. J. Pharmacol.

DESIPRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Sawynok et al., 1999, Peripheral antinociceptive actions of desipramine and fluoxetine in an inflammatory and neuropathic pain test in the rat., Pain

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

CLEMASTINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

Dorsch et al., 1984, Sequential histamine inhalations cause increased bronchial histamine reactivity in guinea pigs: role of platelets, thromboxanes and prostacyclin., Naunyn Schmiedebergs Arch. Pharmacol.

Schran et al., 1996, The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations., J Clin Pharmacol

Taniguchi et al., 1991, Inhibitory effects of histamine H1 receptor blocking drugs on metabolic activations of neutrophils., J. Pharmacobio-dyn.

CARIPRAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

McCormack, 2015, Cariprazine: First Global Approval., Drugs

METHDILAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:

Chattopadhyay et al., 1998, Altered membrane permeability as the basis of bactericidal action of methdilazine., J. Antimicrob. Chemother.

Dasgupta et al., 2010, Experimental analyses of synergistic combinations of antibiotics with a recently recognised antibacterial agent, lacidipine., Eur. J. Clin. Microbiol. Infect. Dis.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

MEQUITAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Wiseman et al., 1996, Ebastine. a review of its pharmacological properties and clinical efficacy in the treatment of allergic disorders., Drugs

Wang et al., 2002, Ketoconazole potentiates terfenadine-induced apoptosis in human Hep G2 cells through inhibition of cytochrome p450 3A4 activity., J. Cell. Biochem.

Nicholson et al., 1983, The H1-antagonist mequitazine: studies on performance and visual function., Eur. J. Clin. Pharmacol.

CHLOROPYRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Kurenova et al., 2009, Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo., J. Med. Chem.

DEXBROMPHENIRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

McLeod et al., 1998, Antitussive action of antihistamines is independent of sedative and ventilation activity in the guinea pig., Pharmacology

Onaran et al., 1990, Kinetics of antagonism at histamine-H1 receptors in isolated rabbit arteries., Naunyn Schmiedebergs Arch. Pharmacol.

Bökesoy et al., 1991, Atypical Schild plots with histamine H1 receptor agonists and antagonists in the rabbit aorta., Eur. J. Pharmacol.

DOXEPIN HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.

CLOZAPINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Trial Name -

Publications:

Leysen et al., 1994, Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity., J Clin Psychiatry

Roegge et al., 2007, Histamine H1 receptor involvement in prepulse inhibition and memory function: relevance for the antipsychotic actions of clozapine., Pharmacol. Biochem. Behav.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

AZATADINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Haria et al., 1994, Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders., Drugs

Clissold et al., 1989, Loratadine. A preliminary review of its pharmacodynamic properties and therapeutic efficacy., Drugs

Singh et al., 1998, Causal prophylactic activity of antihistaminic agents against Plasmodium yoelii nigeriensis infection in Swiss mice., Acta Trop.

PHENINDAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Witek et al., 1992, The effects of phenindamine tartrate on sleepiness and psychomotor performance., J. Allergy Clin. Immunol.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

LEVOMEPROMAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Hals et al., 1988, Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites., Life Sci.

HISTAMINE HRH1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? True

Publications:

Han et al., 2006, Phospholipase Cbeta 3 mediates the scratching response activated by the histamine H1 receptor on C-fiber nociceptive neurons., Neuron

Spahr et al., 2007, Histamine H1 blocker hydroxyzine improves sleep in patients with cirrhosis and minimal hepatic encephalopathy: a randomized controlled pilot trial., Am. J. Gastroenterol.

Tanimoto et al., 2007, Histamine upregulates the expression of inducible nitric oxide synthase in human intimal smooth muscle cells via histamine H1 receptor and NF-kappaB signaling pathway., Arterioscler. Thromb. Vasc. Biol.

BETAHISTINE HRH1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name OBE101,Histalean

Novel drug target Established target

Publications:

Lacour et al., 2001, Histamine and betahistine in the treatment of vertigo: elucidation of mechanisms of action., CNS Drugs

Barak, 2008, Betahistine: what's new on the agenda?, Expert Opin Investig Drugs

PYRILAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem

Jongejan A et al., 2005, Linking agonist binding to histamine H1 receptor activation., Nat Chem Biol

Parsons et al., 2006, Histamine and its receptors., Br. J. Pharmacol.

FLUNARIZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Taylor et al., 1986, Interactions of verapamil, D 600, flunarizine and nifedipine with cerebral histamine-receptors., Neurochem. Int.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

TRIPELENNAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

Ohta et al., 1999, Role of endogenous serotonin and histamine in the pathogenesis of gastric mucosal lesions in unanaesthetised rats with a single treatment of compound 48/80, a mast cell degranulator., Pharmacol. Res.

Sansone, Antihistaminic-opioid combination: effect on locomotor activity in mice., Pol J Pharmacol Pharm

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

ACEPROMETAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Mercier et al., 1974, Electro-encephalographic study on the action of the combination meprobamate-aceprometazine on various cerebral systems., Arzneimittelforschung

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

DESLORATADINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Li J et al., 2020, Human H1 receptor (HRH1) gene polymorphism is associated with the severity of side effects after desloratadine treatment in Chinese patients with chronic spontaneous uticaria., Pharmacogenomics J

Simons et al., 2003, Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis., J. Allergy Clin. Immunol.

Cieślewicz et al., 1995, [Effect of loratadine, selective antagonist of histamine H1 receptors, on histamine-induced bronchoconstriction]., Pneumonol Alergol Pol

FEXOFENADINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name fexofenadine + ps/

Specific Action of the Ligand Antagonist

Publications:

Abbas et al., 2004, A novel membrane sensor for histamine H1-receptor antagonist "fexofenadine"., Anal Sci

Grzelewska-Rzymowska et al., 2003, [Effect of fexofenadine--selective antagonist of histamine receptor (H1) on histamine-induced bronchoconstriction]., Pol. Merkur. Lekarski

Markham et al., 1998, Fexofenadine., Drugs

TRIPROLIDINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Ziganshina et al., 1996, Acute paw oedema formation induced by ATP: re-evaluation of the mechanisms involved., Inflamm. Res.

Estelle et al., 1999, H1-receptor antagonists: safety issues., Ann. Allergy Asthma Immunol.

Claro et al., 1986, Phosphoinositide hydrolysis mediated by histamine H1-receptors in rat brain cortex., Eur. J. Pharmacol.

RISPERIDONE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.

Keks et al., 1999, Risperidone (Risperdal): clinical experience with a new antipsychosis drug., Expert Opin Investig Drugs

Schreiber et al., 1997, Augmentation of opioid induced antinociception by the atypical antipsychotic drug risperidone in mice., Neurosci. Lett.

CINNARIZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Paton et al., Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines)., Clin Pharmacokinet

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

LEVOCABASTINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Sugimoto et al., 1999, Effects of levocabastine on lipid mediator release from guinea pig lung fragments., Acta Med. Okayama

Chalon et al., 1996, Molecular cloning of a levocabastine-sensitive neurotensin binding site., FEBS Lett.

Betancur et al., 1998, Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain., Eur. J. Pharmacol.

DOXYLAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

METHYLPROMAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Santos et al., 1995, Blockers for excitatory effects of achatin-I, a tetrapeptide having a D-phenylalanine residue, on a snail neurone., Eur. J. Pharmacol.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

CHLOPHEDIANOL HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

TERFENADINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

Wood-Baker et al., 1995, A double-blind, placebo controlled study of the effect of the specific histamine H1-receptor antagonist, terfenadine, in chronic severe asthma., Br J Clin Pharmacol

Salata et al., 1995, Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine., Circ. Res.

Rafferty et al., 1987, Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways., Am. Rev. Respir. Dis.

TRAZODONE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Noguchi et al., 1992, The suppression of olfactory bulbectomy-induced muricide by antidepressants and antihistamines via histamine H1 receptor blocking., Physiol. Behav.

Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

CARBINOXAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Oishi et al., 1994, Comparison of the effects of eleven histamine H1-receptor antagonists on monoamine turnover in the mouse brain., Naunyn Schmiedebergs Arch. Pharmacol.

Ramadan et al., 2006, Spectrophotometric determination of carbinoxamine maleate in pharmaceutical formulations by ternary complex formation with Cu(II) and eosin., Anal. Biochem.

HYDROXYZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

inverse agonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Antagonist

Publications:

Spahr et al., 2007, Histamine H1 blocker hydroxyzine improves sleep in patients with cirrhosis and minimal hepatic encephalopathy: a randomized controlled pilot trial., Am. J. Gastroenterol.

Snowman et al., 1990, Cetirizine: actions on neurotransmitter receptors., J. Allergy Clin. Immunol.

Sakaguchi et al., 2008, Hydroxyzine, a first generation H(1)-receptor antagonist, inhibits human ether-a-go-go-related gene (HERG) current and causes syncope in a patient with the HERG mutation., J. Pharmacol. Sci.

MECLIZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Taniguchi et al., 1991, Inhibitory effects of histamine H1 receptor blocking drugs on metabolic activations of neutrophils., J. Pharmacobio-dyn.

Martins et al., 1992, Interference of cetirizine with the late eosinophil accumulation induced by either PAF or compound 48/80., Br. J. Pharmacol.

Oishi et al., 1994, Comparison of the effects of eleven histamine H1-receptor antagonists on monoamine turnover in the mouse brain., Naunyn Schmiedebergs Arch. Pharmacol.

MIANSERIN HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Nowak et al., 1983, Interaction between mianserin, an antidepressant drug, and central H1- and H2-histamine-receptors: in vitro and in vivo studies and radioreceptor assay., Neuropharmacology

Grinshpoon et al., 2000, Beneficial effect of the addition of the 5-HT 2A/2C and alpha2 antagonist mianserin to ongoing haloperidol treatment in drug-resistant chronically hospitalized schizophrenic patients., Eur. Psychiatry

Csaba et al., 2003, Prolonged effect of the tricyclic antidepressant, mianserin on the serotonin and histamine content of young rats' white blood cells and mast cells. A case of late-imprinting., Pharmacol. Res.

OLANZAPINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

Publications:

Altschuler et al., 2005, Using histamine (H1) antagonists, in particular atypical antipsychotics, to treat anemia of chronic disease via interleukin-6 suppression., Med. Hypotheses

Poyurovsky et al., 2005, The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients., Int Clin Psychopharmacol

Uchida et al., 2007, Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine., Life Sci.

LORATADINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Specific Action of the Ligand Antagonist

Publications:

Tamura et al., 2005, Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice., Pharmacology

Baroody et al., 2000, Antiallergic effects of H1-receptor antagonists., Allergy

Cieślewicz et al., 1995, [Effect of loratadine, selective antagonist of histamine H1 receptors, on histamine-induced bronchoconstriction]., Pneumonol Alergol Pol

ZIPRASIDONE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.

Arnt, 1995, Differential effects of classical and newer antipsychotics on the hypermotility induced by two dose levels of D-amphetamine., Eur. J. Pharmacol.

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

ASTEMIZOLE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

Publications:

Howarth et al., 1984, Astemizole, a potent histamine H1-receptor antagonist: effect in allergic rhinoconjunctivitis, on antigen and histamine induced skin weal responses and relationship to serum levels., Br J Clin Pharmacol

Krstenansky et al., 1987, Astemizole: a long-acting, nonsedating antihistamine., Drug Intell Clin Pharm

Llenas et al., 1999, Cardiotoxicity of histamine and the possible role of histamine in the arrhythmogenesis produced by certain antihistamines., Drug Saf

ANTAZOLINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Swiader et al., Effect of histamine receptor antagonists on aminophylline-induced seizures and lethality in mice., Pharmacol Rep

CHLORPHENIRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Nicholson et al., 1991, Sedation and histamine H1-receptor antagonism: studies in man with the enantiomers of chlorpheniramine and dimethindene., Br. J. Pharmacol.

Salata et al., 1995, Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine., Circ. Res.

Hasenöhrl et al., 2001, Comparison of intra-accumbens injection of histamine with histamine H1-receptor antagonist chlorpheniramine in effects on reinforcement and memory parameters., Behav. Brain Res.

MAPROTILINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Noguchi et al., 1992, The suppression of olfactory bulbectomy-induced muricide by antidepressants and antihistamines via histamine H1 receptor blocking., Physiol. Behav.

Kanba et al., 1984, Histamine H1 receptors in human brain labelled with [3H]doxepin., Brain Res.

Cavero et al., 1981, Effects of mianserin, desipramine and maprotiline on blood pressure responses evoked by acetylcholine, histamine and 5-hydroxytryptamine in rats., Br. J. Pharmacol.

CHLORPROMAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Palmer et al., 1978, Histamine-, norepinephrine-, and dopamine-sensitive central adenylate cyclases: effects of chlorpromazine derivatives and butaclamol., Arch Int Pharmacodyn Ther

Church et al., 1983, The characteristics of inhibition of histamine release from human lung fragments by sodium cromoglycate, salbutamol and chlorpromazine., Br. J. Pharmacol.

Hals et al., 1988, Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites., Life Sci.

AZELASTINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Azelastine

Novel drug target Established target

Trial Name azelastine hydrochloride nasal spray,Astepro

Publications:

Golden et al., 1999, Efficacy and safety of azelastine nasal spray for the treatment of allergic rhinitis., J Am Osteopath Assoc

Casale, 1989, The interaction of azelastine with human lung histamine H1, beta, and muscarinic receptor-binding sites., J. Allergy Clin. Immunol.

Antépara et al., [Investigation of the efficacy and tolerability of azelastine nasal spray versus ebastine tablets in patients with seasonal allergic rhinitis]., Allergol Immunopathol (Madr)

EMEDASTINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Murota et al., 2008, Emedastine difumarate inhibits histamine-induced collagen synthesis in dermal fibroblasts., J Investig Allergol Clin Immunol

Corrado et al., 2004, Clinical study of the therapeutic efficacy and safety of emedastine difumarate versus terfenadine in the treatment of seasonal allergic rhinitis., Arzneimittelforschung

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

CHLORPROTHIXENE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Ding P et al., 2017, PTS: a pharmaceutical target seeker., Database (Oxford)

DIPHENYLPYRALINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Taniguchi et al., 1991, Inhibitory effects of histamine H1 receptor blocking drugs on metabolic activations of neutrophils., J. Pharmacobio-dyn.

Lapa et al., 2005, Diphenylpyraline, a histamine H1 receptor antagonist, has psychostimulant properties., Eur. J. Pharmacol.

Nakai et al., 1991, Decreased histamine H1 receptors in the frontal cortex of brains from patients with chronic schizophrenia., Biol. Psychiatry

CHLORCYCLIZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Enright et al., 2010, Effects of the histamine H1 antagonist chlorcyclizine on rat fetal palate development., Birth Defects Res. B Dev. Reprod. Toxicol.

QUETIAPINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

BEPOTASTINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name bepotastine besilate,Bepreve, Talion

Novel drug target Established target

Publications:

Andoh et al., 2006, Suppression by bepotastine besilate of substance P-induced itch-associated responses through the inhibition of the leukotriene B4 action in mice., Eur. J. Pharmacol.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

ESMIRTAZAPINE HRH1

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Publications:

Ivgy-May et al., 2015, Esmirtazapine in non-elderly adult patients with primary insomnia: efficacy and safety from a randomized, 6-week sleep laboratory trial., Sleep Med.

OLOPATADINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name olopatadine hydrochloride,Patanase

Novel drug target Established target

Publications:

Tamura et al., 2005, Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice., Pharmacology

Ohmori et al., 2004, Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug., Arzneimittelforschung

Kaliner et al., Comprehensive review of olopatadine: the molecule and its clinical entities., Allergy Asthma Proc

ORPHENADRINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Rumore et al., 1985, Analgesic effects of antihistaminics., Life Sci.

NORTRIPTYLINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Sadava et al., 1984, Tricyclic antidepressant drugs affect histamine receptors in human leukocytes., Life Sci.

Taylor JE et al., 1980, High affinity binding of tricyclic antidepressants to histamine H1-receptors: fact and artifact., Eur J Pharmacol

ILOPERIDONE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name iloperidone,Fanapt, Fiapta, Zomaril

Novel drug target Established target

Publications:

Bobo, 2013, Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults., Expert Rev Clin Pharmacol

BUCLIZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

TESMILIFENE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Brandes et al., 1987, Histamine and growth: interaction of antiestrogen binding site ligands with a novel histamine site that may be associated with calcium channels., Cancer Res.

DIMETHINDENE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Moree et al., 2010, Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia., Bioorg. Med. Chem. Lett.

Pfaff et al., 1995, The (S)-(+)-enantiomer of dimethindene: a novel M2-selective muscarinic receptor antagonist., Eur. J. Pharmacol.

BENZQUINAMIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Niemegeers, 1982, Antiemetic specificity of dopamine antagonists., Psychopharmacology (Berl.)

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

AMITRIPTYLINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Antagonism of [3H]mepyramine binding

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Kachur JF et al., 1988, Antihistaminic and antimuscarinic effects of amitriptyline on guinea pig ileal electrolyte transport and muscle contractility in vitro., J Pharmacol Exp Ther

Richelson E, 1979, Tricyclic antidepressants and histamine H1 receptors., Mayo Clin Proc

ISOTHIPENDYL HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Moreau et al., 1995, Phototoxic and photoprotective effects of topical isothipendyl., Photodermatol Photoimmunol Photomed

LEVOCETIRIZINE HRH1

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Trial Name levocetirizine dihydrochloride,Xusal, Xyzal

Novel drug target Established target

Publications:

Devillier et al., 2008, Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review., Clin Pharmacokinet

Ferrer, 2011, Pharmacokinetic evaluation of levocetirizine., Expert Opin Drug Metab Toxicol

TRIMIPRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Berger et al., 1996, Trimipramine: a challenge to current concepts on antidepressives., Eur Arch Psychiatry Clin Neurosci

PROMAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Hals et al., 1988, Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites., Life Sci.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

BUTRIPTYLINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.

Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.

Wander et al., 1986, Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro., Eur. J. Pharmacol.

TIAPRIDE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Scatton et al., 2001, The preclinical pharmacologic profile of tiapride., Eur. Psychiatry
BILASTINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Wang et al., 2016, Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine., Ther Clin Risk Manag

MIRTAZAPINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Vande Griend JP et al., 2012, Histamine-1 receptor antagonism for treatment of insomnia., J Am Pharm Assoc (2003)

Salvi V et al., 2016, H1-histamine receptor affinity predicts weight gain with antidepressants., Eur Neuropsychopharmacol

BENZATROPINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Kulkarni et al., 2006, Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors., Bioorg. Med. Chem.

ARIPIPRAZOLE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

PALIPERIDONE HRH1

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Publications:

Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.

Megens et al., 1994, Survey on the pharmacodynamics of the new antipsychotic risperidone., Psychopharmacology (Berl.)

Cohen, Risperidone., Pharmacotherapy

HALOPERIDOL HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
AMOXAPINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.
PROCHLORPERAZINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Isah AO et al., 1991, Clinical pharmacology of prochlorperazine in healthy young males., Br J Clin Pharmacol

ESCITALOPRAM HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Publications:

Fabre et al., [Mechanisms of action of antidepressants: new data from Escitalopram]., Encephale

Bareggi et al., 2007, The use of escitalopram beyond major depression: pharmacological aspects, efficacy and tolerability in anxiety disorders., Expert Opin Drug Metab Toxicol

Sanchez C et al., 2014, A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike?, Int Clin Psychopharmacol

IMIPRAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
CITALOPRAM HRH1

Interaction Types & Directionality:

binder

Interaction Info:

Publications:

Bareggi et al., 2007, The use of escitalopram beyond major depression: pharmacological aspects, efficacy and tolerability in anxiety disorders., Expert Opin Drug Metab Toxicol
TOLAZOLINE HRH1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Roll et al., 1993, [Interaction of tolazoline and cimetidine in persistent fetal circulation of the newborn infant]., Monatsschr Kinderheilkd
PEROSPIRONE HRH1

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Publications:

Kishi T et al., 2013, Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials., CNS Drugs
PIZOTYLINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol

THONZYLAMINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

SCUDI JV et al., 1948, Pharmacologic characteristics of neohetramine, a new antihistaminic drug., J Allergy

AARON TH et al., 1948, Neohetramine and thephorin; two new antihistaminic drugs., Can Med Assoc J

PAROXETINE HRH1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Westenberg HG et al., 2006, Tolerability and safety of fluvoxamine and other antidepressants., Int J Clin Pract

LAMOTRIGINE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Vinod KY et al., 2002, Lamotrigine induced selective changes in 5-HT(1A) receptor mediated response in rat brain., Neurochem Int

Bourin M et al., 2005, Evidence for the activity of lamotrigine at 5-HT(1A) receptors in the mouse forced swimming test., J Psychiatry Neurosci

Abelaira HM et al., 2012, Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats., Pharmacol Biochem Behav

LORPIPRAZOLE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Jarema M et al., 2011, [Trazodon--the antidepressant: mechanism of action and its position in the treatment of depression]., Psychiatr Pol
LOXAPINE HRH1

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
ZUCLOPENTHIXOL HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:
GSK-1004723 HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name GSK-1004723

Novel drug target Established target

Publications:
PEMIROLAST HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
THIETHYLPERAZINE HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:
VAPITADINE HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name vapitadine dihydrochloride,Hivenyl

Novel drug target Established target

Publications:
BIPERIDEN HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Vasudevan SR et al., 2012, Shape-based reprofiling of FDA-approved drugs for the H₁ histamine receptor., J Med Chem
chembl:CHEMBL1923521 HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem
OCAPERIDONE HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
(S)-(+)-DIMETHINDENE HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL95051 HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL491889 HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CAREBASTINE HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL261551 HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
OXATOMIDE HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ETHOPROPAZINE HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TRANILAST HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
NOBERASTINE HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
LATREPIRDINE HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL318235 HRH1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000196639
- Version: 101_38
Alternate Names:

HRH1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P35367
- Version: 11-September-2012
Alternate Names:

HRH1_HUMAN Uniprot Id

HISTAMINE H1 RECEPTOR Uniprot Protein Name

HRH1 Uniprot Gene Name

Gene Info:

Interpro Acc IPR000276

Uniprot Status Swiss-Prot

Uniprot Evidence 1: Evidence at protein level

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
GuideToPharmacologyGenes: 262
- Version: 4-March-2015
Alternate Names:

histamine receptor H1 HUGO Gene Name

5182 HUGO Gene ID

HRH1 Gene Symbol

Gene Info:

GuideToPharmacology Gene Category Name Histamine receptors

GuideToPharmacology Gene Category ID 33

GuideToPharmacology Gene Type gpcr

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TEND: P35367
- Version: 01-August-2011
Alternate Names:

HRH1 Gene Symbol

ENSG00000196639 Ensembl Gene Id

HRH1_HUMAN Uniprot Id

Gene Info:

Transmembrane Helix Count 7

Target Subclass Rhodopsin

Target Subclass GPCR

Publications:
TdgClinicalTrial: P35367
- Version: January-2014
Alternate Names:

HRH1 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
RussLampel: ENSG00000196639
- Version: 26-July-2011
Alternate Names:

HISTAMINE H1 RECEPTOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P35367] Description

HRH1 Display Id

ENSG00000196639 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

PharmGKB: HRH1

Version: 18-August-2020

Alternate Names:

PA29456 PharmGKB ID

Gene Info:

Publications:

Li J et al., 2020, Human H1 receptor (HRH1) gene polymorphism is associated with the severity of side effects after desloratadine treatment in Chinese patients with chronic spontaneous uticaria., Pharmacogenomics J

TTD: Histamine H1 receptor
- Version: 2020.06.01
Alternate Names:

H1R TTD Gene Abbreviation

T77913 TTD Target ID

Gene Info:

Publications:

Lacour M et al., 2007, Betahistine in the treatment of Ménière's disease., Neuropsychiatr Dis Treat

DrugBank: BE0000442

Version: 5.1.7

Alternate Names:

HRH1 DrugBank Gene Name

P35367 UniProt Accession

3269 Entrez Gene Id

Gene Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.

Schran et al., 1996, The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations., J Clin Pharmacol

DTC: HRH1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Vasudevan SR et al., 2012, Shape-based reprofiling of FDA-approved drugs for the H₁ histamine receptor., J Med Chem

Jongejan A et al., 2005, Linking agonist binding to histamine H1 receptor activation., Nat Chem Biol

de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem

HingoraniCasas: ENSG00000196639
- Version: 31-May-2017
Alternate Names:

ENSG00000196639 Gene Symbol

HRH1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: HRH1
- Version: chembl_23
Alternate Names:

HRH1 GENE_SYMBOL

Histamine H1 receptor UNIPROT

H1R UNIPROT

Gene Info:

Publications:
GuideToPharmacologyInteractions: ENSG00000196639
- Version: 20-July-2020
Alternate Names:

H1 receptor GuideToPharmacology Name

P35367 UniProtKB ID

Gene Info:

Publications:
dGene: HRH1
- Version: 27-Jun-2013
Alternate Names:

3269 Gene ID

H1-R dGene Synonym

hisH1 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
GO: HRH1
- Version: 05-September-2020
Alternate Names:

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

Details of the Assay for Interaction	Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Trial Name	-
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Mechanism of Interaction	Histamine H1 receptor antagonist
Direct Interaction	yes

Direct Interaction?	False
Endogenous Drug?	False
Specific Action of the Ligand	Antagonist

Mechanism of Interaction	Histamine H1 receptor agonist
Direct Interaction	yes

Specific Action of the Ligand	Agonist
Endogenous Drug?	False
Direct Interaction?	False

Specific Action of the Ligand	Inverse agonist
Endogenous Drug?	False

Details of the Assay for Interaction	Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Trial Name	cetirizine HCl,Zyrtec
Novel drug target	Established target
Direct Interaction?	True

Trial Name	ketotifen fumarate,Zaditen, Zaditor
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Trial Name	Silenor (SO-101)
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Specific Action of the Ligand	Full agonist
Endogenous Drug?	True

Trial Name	OBE101,Histalean
Novel drug target	Established target

Trial Name	Azelastine
Novel drug target	Established target
Trial Name	azelastine hydrochloride nasal spray,Astepro

Trial Name	bepotastine besilate,Bepreve, Talion
Novel drug target	Established target

Trial Name	olopatadine hydrochloride,Patanase
Novel drug target	Established target

Trial Name	iloperidone,Fanapt, Fiapta, Zomaril
Novel drug target	Established target

Details of the Assay for Interaction	Antagonism of [<sup>3</sup>H]mepyramine binding
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Trial Name	levocetirizine dihydrochloride,Xusal, Xyzal
Novel drug target	Established target

Trial Name	vapitadine dihydrochloride,Hivenyl
Novel drug target	Established target

HRH1 Gene Record

HRH1 3269 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Details of the Assay for Interaction Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells. Specific Action of the Ligand Antagonist Endogenous Drug? False

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Specific Action of the Ligand Antagonist

Publications: Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name - Specific Action of the Ligand Antagonist

Publications: Leza et al., 1990, H1- and H2-histamine receptor blockers and opiate analgesia in mice., Methods Find Exp Clin Pharmacol Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Mechanism of Interaction Histamine H1 receptor antagonist

Publications: Halpert et al., 2002, Mechanisms and abuse liability of the anti-histamine dimenhydrinate., Neurosci Biobehav Rev Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Mechanism of Interaction Histamine H1 receptor antagonist

Publications: Simons et al., 2011, Histamine and H1-antihistamines: celebrating a century of progress., J. Allergy Clin. Immunol.

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Trial Name Asenapine

Publications: Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford) Citrome, 2011, Role of sublingual asenapine in treatment of schizophrenia., Neuropsychiatr Dis Treat

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

Publications: Merlos M et al., 1997, Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF)., J Pharmacol Exp Ther

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

Publications: Gillman, 2007, Tricyclic antidepressant pharmacology and therapeutic drug interactions updated., Br. J. Pharmacol.

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H1 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H1 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Antagonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H1 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histamine H1 receptor antagonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H1 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histamine H1 receptor antagonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histamine H1 receptor antagonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H1 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Inverse agonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H1 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H1 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histamine H1 receptor antagonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H1 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H1 receptor antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Antagonist

Publications:

Leza et al., 1990, H1- and H2-histamine receptor blockers and opiate analgesia in mice., Methods Find Exp Clin Pharmacol

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:

Halpert et al., 2002, Mechanisms and abuse liability of the anti-histamine dimenhydrinate., Neurosci Biobehav Rev

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Histamine H1 receptor antagonist

Publications:

Simons et al., 2011, Histamine and H1-antihistamines: celebrating a century of progress., J. Allergy Clin. Immunol.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Trial Name Asenapine

Publications:

Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)

Citrome, 2011, Role of sublingual asenapine in treatment of schizophrenia., Neuropsychiatr Dis Treat

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Merlos M et al., 1997, Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF)., J Pharmacol Exp Ther

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

Gillman, 2007, Tricyclic antidepressant pharmacology and therapeutic drug interactions updated., Br. J. Pharmacol.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inverse agonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor agonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

HRH1_HUMAN	Uniprot Id
HISTAMINE H1 RECEPTOR	Uniprot Protein Name
HRH1	Uniprot Gene Name

histamine receptor H1	HUGO Gene Name
5182	HUGO Gene ID
HRH1	Gene Symbol

HISTAMINE H1 RECEPTOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P35367]	Description
HRH1	Display Id
ENSG00000196639	Ensembl Gene Id

HRH1	DrugBank Gene Name
P35367	UniProt Accession
3269	Entrez Gene Id

H<sub>1</sub> receptor	GuideToPharmacology Name
P35367	UniProtKB ID