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HRH1 Gene Record

  • Summary
  • Interactions
  • Claims
  • 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.
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    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.
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    Kaliner et al., Comprehensive review of olopatadine: the molecule and its clinical entities., Allergy Asthma Proc
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    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.
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    Bobo, 2013, Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults., Expert Rev Clin Pharmacol
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    Niemegeers, 1982, Antiemetic specificity of dopamine antagonists., Psychopharmacology (Berl.)
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    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
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    Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
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    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)
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    Megens et al., 1994, Survey on the pharmacodynamics of the new antipsychotic risperidone., Psychopharmacology (Berl.)
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    Isah AO et al., 1991, Clinical pharmacology of prochlorperazine in healthy young males., Br J Clin Pharmacol
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  • 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