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]
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
Transmembrane Helix Count	7
Target Subclass	Rhodopsin
Target Subclass	GPCR
Target Main Class	Receptors
Target Class	Receptors
Gene Biotype	PROTEIN_CODING

(10 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.)
Richelson E, 1979, Tricyclic antidepressants and histamine H1 receptors., Mayo Clin Proc
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
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.
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)
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)
Salvi V et al., 2016, H1-histamine receptor affinity predicts weight gain with antidepressants., Eur Neuropsychopharmacol
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
Cicek E et al., 2017, Bilateral Pretibial Edema Associated with Paliperidone Palmitate Long-acting Injectable: A Case Report., Clin Psychopharmacol Neurosci
Gilday E et al., 2012, Clinical pharmacology of paliperidone palmitate a parenteral long-acting formulation for the treatment of schizophrenia., Rev Recent Clin Trials
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
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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
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Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
Westenberg HG et al., 2006, Tolerability and safety of fluvoxamine and other antidepressants., Int J Clin Pract
AARON TH et al., 1948, Neohetramine and thephorin; two new antihistaminic drugs., Can Med Assoc J
SCUDI JV et al., 1948, Pharmacologic characteristics of neohetramine, a new antihistaminic drug., J Allergy
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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
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
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Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.

EMEDASTINE HRH1

Interaction Score: 3.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18714531 15553105 11752352 7714409 9747899 19558341 7714410

Sources:
DrugBank TdgClinicalTrial TEND TTD
TRIPELENNAMINE HRH1

Interaction Score: 3.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
10208755 3253717 11752352 6759742 996853 9226736

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
MEQUITAZINE HRH1

Interaction Score: 3.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8808167 12244568 6418550 7650688 11752352 7511558 9454781

Sources:
DrugBank TdgClinicalTrial TEND TTD
METHDILAZINE HRH1

Interaction Score: 3.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction Histamine H1 receptor antagonist

PMIDs:
9700532 20012879 17016423 17139284 11752352

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND TTD
AZATADINE HRH1

Interaction Score: 2.78

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7528133 2523301 9638277 11752352 2568212

Sources:
DrugBank TdgClinicalTrial TEND TTD
CHLOPHEDIANOL HRH1

Interaction Score: 2.47

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 11752352 2905706

Sources:
DrugBank TdgClinicalTrial TEND TTD
ACEPROMETAZINE HRH1

Interaction Score: 2.47

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
4406367 17016423 17139284 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD
TRIPROLIDINE HRH1

Interaction Score: 2.32

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
8907591 10582735 3011460 2568212 10493107 7913608 2866055 7214150 11752352 7853212

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
PHENINDAMINE HRH1

Interaction Score: 2.16

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
11752352 1360991 17016423 1686618 7650688

Sources:
DrugBank TTD
BROMODIPHENHYDRAMINE HRH1

Interaction Score: 2.16

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD
BEPOTASTINE HRH1

Interaction Score: 1.85

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name bepotastine besilate,Bepreve, Talion

Novel drug target Established target

PMIDs:
16914135 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD
ALCAFTADINE HRH1

Interaction Score: 1.85

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Histamine H1 receptor antagonist

PMIDs:
22035879

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND TTD
METHYLPROMAZINE HRH1

Interaction Score: 1.85

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7713167 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD
LEVOCABASTINE HRH1

Interaction Score: 1.54

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10631382 8647296 9551716 11915520 9627096 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD
FEXOFENADINE HRH1

Interaction Score: 1.54

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name fexofenadine + ps/

Specific Action of the Ligand Antagonist

PMIDs:
15352500 12712828 9506246 18336052 15286093 18797058 19545214 10864400 11752352 10597865

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
DEXBROMPHENIRAMINE HRH1

Interaction Score: 1.54

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
9691225 1970615 1680053 11752352 19085565 7714410

Sources:
DrugBank TdgClinicalTrial TEND TTD
CARBINOXAMINE HRH1

Interaction Score: 1.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11752352 7513381 16574052 1143714 19761204

Sources:
DrugBank TdgClinicalTrial TEND TTD
LEVOCETIRIZINE HRH1

Interaction Score: 1.23

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Trial Name levocetirizine dihydrochloride,Xusal, Xyzal

Novel drug target Established target

PMIDs:
18336052 21639816

Sources:
DrugBank TdgClinicalTrial
DESLORATADINE HRH1

Interaction Score: 1.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
31406237 12642846 7581058 18336052 8174605 15564772 18797058 11752352 17902729

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD
PHENIRAMINE HRH1

Interaction Score: 1.23

Interaction Types & Directionality:

antagonist (inhibitory)

inverse agonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8835636 2567596 20027159 14506317 11752352 17016423 7714410 11526976

Sources:
DrugBank TdgClinicalTrial TEND TTD
DIPHENYLPYRALINE HRH1

Interaction Score: 1.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
1678430 15627433 1912125 18977145 11752352 17016423 17139284

Sources:
DrugBank TdgClinicalTrial TEND TTD
BUCLIZINE HRH1

Interaction Score: 1.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD
AZELASTINE HRH1

Interaction Score: 1.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Azelastine

Novel drug target Established target

Trial Name azelastine hydrochloride nasal spray,Astepro

PMIDs:
10478514 2540229 9585822 8829888 11752352 17723160 19209282 21381763

Sources:
DTC DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
DIMENHYDRINATE HRH1

Interaction Score: 1.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Histamine H1 receptor antagonist

PMIDs:
11835984 11752352

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND TTD
CYCLIZINE HRH1

Interaction Score: 1.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Antagonist

PMIDs:
1983158 11752352

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
PEMIROLAST HRH1

Interaction Score: 0.93

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND TTD
ACRIVASTINE HRH1

Interaction Score: 0.93

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
DrugBank ChemblInteractions TTD
KETOTIFEN HRH1

Interaction Score: 0.93

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name ketotifen fumarate,Zaditen, Zaditor

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
8836617 8101246 7893266 16404130 11752352 1434122 18490184

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
CETIRIZINE HRH1

Interaction Score: 0.8

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name cetirizine HCl,Zyrtec

Novel drug target Established target

Endogenous Drug? False

PMIDs:
12787835 15942272 15286093 14505791 11752352 10597865 23867423 14680442

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
CHEMBL1923521 HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22007643

Sources:
DTC
DEXCHLORPHENIRAMINE MALEATE HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
DrugBank ChemblInteractions
VAPITADINE HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name vapitadine dihydrochloride,Hivenyl

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TTD
BILASTINE HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
27110120

Sources:
DrugBank
ISOTHIPENDYL HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
8546983

Sources:
DrugBank
DIMETHINDENE HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
20800486 8608784

Sources:
DrugBank TTD
RUPATADINE HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
8996188

Sources:
DrugBank GuideToPharmacology TTD
CHLORCYCLIZINE HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
21058326

Sources:
DrugBank
LY2624803 HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H1 receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions TTD
BETAHISTINE HRH1

Interaction Score: 0.62

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name OBE101,Histalean

Novel drug target Established target

PMIDs:
11700150 18447604

Sources:
DrugBank TdgClinicalTrial
CHLORPHENIRAMINE HRH1

Interaction Score: 0.57

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
1686208 8001268 11640974 7648771 11752352 11736858

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
DOXYLAMINE HRH1

Interaction Score: 0.54

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD
CLEMASTINE HRH1

Interaction Score: 0.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
6387510 8930778 1678430 2890562 7513381 6701456 6449094 11752352 1266718 4074605

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
BROMPHENIRAMINE HRH1

Interaction Score: 0.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7855217 10212017 1970615 1680053 11752352 7714410

Sources:
DrugBank TdgClinicalTrial TEND TTD
OLOPATADINE HRH1

Interaction Score: 0.5

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name olopatadine hydrochloride,Patanase

Novel drug target Established target

PMIDs:
15942272 15646365 20406593 11496828 20482305 12046981 11752352 20402382 8951675

Sources:
DrugBank TdgClinicalTrial TEND TTD
PYRILAMINE HRH1

Interaction Score: 0.49

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
22007643 16408006 16402096 19544046 19537525 1979798 19552055

Sources:
DTC DrugBank GuideToPharmacology TTD
ANTAZOLINE HRH1

Interaction Score: 0.46

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
16129921

Sources:
DrugBank TTD
DIPHENHYDRAMINE HRH1

Interaction Score: 0.46

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Antagonist

PMIDs:
17329841 17169617 17196194 17390763 2878016 11752352 16702624

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
HYDROXYZINE HRH1

Interaction Score: 0.42

Interaction Types & Directionality:

antagonist (inhibitory)

inverse agonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Antagonist

PMIDs:
17222324 1979798 19057127 18781943 11752352 23330992

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
BUTRIPTYLINE HRH1

Interaction Score: 0.41

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
6086881 9537821 3816971

Sources:
DrugBank
MECLIZINE HRH1

Interaction Score: 0.36

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
1678430 1350745 7513381 1362160

Sources:
DrugBank TdgClinicalTrial TEND

EPINASTINE HRH1

Interaction Score: 0.35

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

PMIDs:
17534605 1972625 11752352

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

BROMPHENIRAMINE MALEATE HRH1

Interaction Score: 0.31

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BROMODIPHENHYDRAMINE HYDROCHLORIDE HRH1

Interaction Score: 0.31

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BUCLIZINE HYDROCHLORIDE HRH1

Interaction Score: 0.31

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

MIZOLASTINE HRH1

Interaction Score: 0.31

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

PMIDs:
None found

Sources:
GuideToPharmacology TTD

HISTAMINE PHOSPHATE HRH1

Interaction Score: 0.31

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Histamine H1 receptor agonist

Direct Interaction yes

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

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

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

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

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

Mechanism of Interaction	Histamine H1 receptor antagonist
Direct Interaction	yes

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

Trial Name	cetirizine HCl,Zyrtec
Novel drug target	Established target
Endogenous Drug?	False

Trial Name	vapitadine dihydrochloride,Hivenyl
Novel drug target	Established target

Trial Name	OBE101,Histalean
Novel drug target	Established target

Trial Name	olopatadine hydrochloride,Patanase
Novel drug target	Established target

Specific Action of the Ligand	Inverse agonist
Endogenous Drug?	False
Direct Interaction?	True

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

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

Mechanism of Interaction	Histamine H1 receptor agonist
Direct Interaction	yes

HRH1 Gene Record

HRH1 3269 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 18714531 15553105 11752352 7714409 9747899 19558341 7714410

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 10208755 3253717 11752352 6759742 996853 9226736

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 8808167 12244568 6418550 7650688 11752352 7511558 9454781

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 9700532 20012879 17016423 17139284 11752352

Sources: DrugBank TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 7528133 2523301 9638277 11752352 2568212

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284 11752352 2905706

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 4406367 17016423 17139284 11752352

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 8907591 10582735 3011460 2568212 10493107 7913608 2866055 7214150 11752352 7853212

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 11752352 1360991 17016423 1686618 7650688

Sources: DrugBank TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284 11752352

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name bepotastine besilate,Bepreve, Talion Novel drug target Established target

PMIDs: 16914135 11752352

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 22035879

Sources: DrugBank TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 7713167 11752352

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10631382 8647296 9551716 11915520 9627096 11752352

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name fexofenadine + ps/ Specific Action of the Ligand Antagonist

PMIDs: 15352500 12712828 9506246 18336052 15286093 18797058 19545214 10864400 11752352 10597865

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 9691225 1970615 1680053 11752352 19085565 7714410

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 11752352 7513381 16574052 1143714 19761204

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: inhibitor (inhibitory) antagonist (inhibitory)

Interaction Info: Trial Name levocetirizine dihydrochloride,Xusal, Xyzal Novel drug target Established target

PMIDs: 18336052 21639816

Sources: DrugBank TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18714531 15553105 11752352 7714409 9747899 19558341 7714410

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
10208755 3253717 11752352 6759742 996853 9226736

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8808167 12244568 6418550 7650688 11752352 7511558 9454781

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction Histamine H1 receptor antagonist

PMIDs:
9700532 20012879 17016423 17139284 11752352

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7528133 2523301 9638277 11752352 2568212

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 11752352 2905706

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
4406367 17016423 17139284 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
8907591 10582735 3011460 2568212 10493107 7913608 2866055 7214150 11752352 7853212

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
11752352 1360991 17016423 1686618 7650688

Sources:
DrugBank TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name bepotastine besilate,Bepreve, Talion

Novel drug target Established target

PMIDs:
16914135 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Histamine H1 receptor antagonist

PMIDs:
22035879

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7713167 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10631382 8647296 9551716 11915520 9627096 11752352

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name fexofenadine + ps/

Specific Action of the Ligand Antagonist

PMIDs:
15352500 12712828 9506246 18336052 15286093 18797058 19545214 10864400 11752352 10597865

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
9691225 1970615 1680053 11752352 19085565 7714410

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11752352 7513381 16574052 1143714 19761204

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Trial Name levocetirizine dihydrochloride,Xusal, Xyzal

Novel drug target Established target

PMIDs:
18336052 21639816

Sources:
DrugBank TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
31406237 12642846 7581058 18336052 8174605 15564772 18797058 11752352 17902729

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

antagonist (inhibitory)

inverse agonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8835636 2567596 20027159 14506317 11752352 17016423 7714410 11526976

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)