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HTR2A Gene Record

  • Summary
  • Interactions
  • Claims
  • HTR2A 3356 Druggable Genome

    Alternate Names:

    3356
    5-HYDROXYTRYPTAMINE RECEPTOR 2A
    HTR2A
    5-HT2A
    HTR2
    182135
    5293
    ENSG00000102468
    OTTHUMG00000016881
    Serotonin receptor 2A
    5-HT-2
    5-HT-2A
    P28223
    5HT2A_HUMAN
    PA193
    5-HYDROXYTRYPTAMINE 2A RECEPTOR (5-HT-2A) (SEROTONIN RECEPTOR 2A) (5- HT-2). [SOURCE:UNIPROT/SWISSPROT;ACC:P28223]
    5-HT 2A receptor
    T32060

    Gene Info:

    Target Main Class Receptors
    Target Subclass Rhodopsin
    Transmembrane Helix Count 7
    Target Subclass GPCR
    Human Readable Name G PROTEIN COUPLED RECEPTOR
    Interpro Acc IPR000276
    Uniprot Status Swiss-Prot
    Uniprot Evidence 1: Evidence at protein level
    Interpro Name GPCR, rhodopsin-like, 7TM
    Interpro Type Family
    Human Readable Name DRUGGABLE GENOME
    Interpro Short Name 7TM_GPCR_Rhodpsn
    Target Class Receptors
    Gene Biotype PROTEIN_CODING
    (8 More Sources)

    Gene Categories: Category Details

    KINASE
    G PROTEIN COUPLED RECEPTOR
    DRUGGABLE GENOME

    Publications:

    Roth et al., 1994, Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors., J. Pharmacol. Exp. Ther.
    Kusumi et al., 2000, Differential effects of subchronic treatments with atypical antipsychotic drugs on dopamine D2 and serotonin 5-HT2A receptors in the rat brain., J Neural Transm (Vienna)
    Yamada et al., 1995, Serotonin2 (5-HT2) receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) inhibits chlorpromazine- and haloperidol-induced hypothermia in mice., Biol. Pharm. Bull.
    Maeda et al., 2014, Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator., J. Pharmacol. Exp. Ther.
    Kongsamut et al., 1996, Iloperidone binding to human and rat dopamine and 5-HT receptors., Eur. J. Pharmacol.
    Hesselink, 2002, Iloperidone (Novartis)., IDrugs
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Serretti et al., Serotonin receptor 2A, 2C, 1A genes and response to lithium prophylaxis in mood disorders., J Psychiatr Res
    Kumar B et al., 2018, Lumateperone: a new treatment approach for neuropsychiatric disorders., Drugs Today (Barc)
    Antkiewicz-Michaluk, The influence of chronic treatment with antidepressant neuroleptics on the central serotonin system., Pol J Pharmacol Pharm
    Wander et al., 1987, Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro., Eur. J. Pharmacol.
    Nash et al., 1994, Effect of the R(-) and S(+) isomers of MDA and MDMA on phosphatidyl inositol turnover in cultured cells expressing 5-HT2A or 5-HT2C receptors., Neurosci. Lett.
    Lyon et al., 1986, 3,4-Methylenedioxymethamphetamine (MDMA): stereoselective interactions at brain 5-HT1 and 5-HT2 receptors., Psychopharmacology (Berl.)
    Leysen et al., 1994, Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity., J Clin Psychiatry
    Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
    Nakamura et al., 2001, Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism., Eur. J. Pharmacol.
    Kobayashi et al., 1996, Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems., Eur. J. Pharmacol.
    Honda et al., 2003, Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors., Eur. J. Pharmacol.
    Mestres J et al., 2011, Linking pharmacology to clinical reports: cyclobenzaprine and its possible association with serotonin syndrome., Clin Pharmacol Ther
    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
    Deeks, 2015, Flibanserin: First Global Approval., Drugs
    Borsini et al., 2002, Pharmacology of flibanserin., CNS Drug Rev
    Invernizzi et al., 2003, Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors., Br. J. Pharmacol.
    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
    McIntyre et al., 2007, A preclinical and clinical rationale for quetiapine in mood syndromes., Expert Opin Pharmacother
    Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.
    Goldstein, 1999, Quetiapine fumarate (Seroquel): a new atypical antipsychotic., Drugs Today
    Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
    Yatham et al., 2005, Atypical antipsychotics in bipolar depression: potential mechanisms of action., J Clin Psychiatry
    Choi et al., 2004, Synthesis, receptor binding and functional studies of mesoridazine stereoisomers., Bioorg. Med. Chem. Lett.
    Rauser et al., 2001, Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor., J. Pharmacol. Exp. Ther.
    Herrick-Davis et al., 2000, Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors., J. Pharmacol. Exp. Ther.
    Hietala et al., 2001, Sertindole is a serotonin 5-HT2c inverse agonist and decreases agonist but not antagonist binding to 5-HT2c receptors after chronic treatment., Psychopharmacology (Berl.)
    Schreiber et al., 1994, Blockade of the discriminative stimulus effects of DOI by MDL 100,907 and the 'atypical' antipsychotics, clozapine and risperidone., Eur. J. Pharmacol.
    Lindström et al., 2006, Sertindole: efficacy and safety in schizophrenia., Expert Opin Pharmacother
    Kasho et al., 1998, Serotonin enhances the production of type IV collagen by human mesangial cells., Kidney Int.
    Bixo et al., 2001, Binding of [3H]paroxetine to serotonin uptake sites and of [3H]lysergic acid diethylamide to 5-HT2A receptors in platelets from women with premenstrual dysphoric disorder during gonadotropin releasing hormone treatment., Psychoneuroendocrinology
    Meyer et al., 2001, The effect of paroxetine on 5-HT(2A) receptors in depression: an [(18)F]setoperone PET imaging study., Am J Psychiatry
    Kato M et al., 2009, 5-HT2A gene variants influence specific and different aspects of antidepressant response in Japanese and Italian mood disorder patients., Psychiatry Res
    Wilkie MJ et al., 2009, Polymorphisms in the SLC6A4 and HTR2A genes influence treatment outcome following antidepressant therapy., Pharmacogenomics J
    Tanaka M et al., 2008, Genetic polymorphisms in the 5-hydroxytryptamine type 3B receptor gene and paroxetine-induced nausea., Int J Neuropsychopharmacol
    Murphy GM Jr et al., 2003, Pharmacogenetics of antidepressant medication intolerance., Am J Psychiatry
    Foster RH et al., 1997, Paroxetine : a review of its pharmacology and therapeutic potential in the management of panic disorder., CNS Drugs
    Newcombe F et al., 1969, Alkaloids of the leaves of Voacanga schweinfurthii Stapf., Planta Med
    Canton et al., 1994, Competitive antagonism of serotonin (5-HT)2C and 5-HT2A receptor-mediated phosphoinositide (PI) turnover by clozapine in the rat: a comparison to other antipsychotics., Neurosci. Lett.
    Costall et al., 1995, Behavioural interactions between 5-hydroxytryptophan, neuroleptic agents and 5-HT receptor antagonists in modifying rodent responding to aversive situations., Br. J. Pharmacol.
    Morisset et al., 1999, Atypical neuroleptics enhance histamine turnover in brain via 5-Hydroxytryptamine2A receptor blockade., J. Pharmacol. Exp. Ther.
    Andree et al., 1986, Differential effect of subchronic treatment with various neuroleptic agents on serotonin2 receptors in rat cerebral cortex., J. Neurochem.
    Burki, 1986, Binding of psychoactive drugs to rat brain amine receptors, measured ex vivo, and their effects on the metabolism of biogenic amines., Naunyn Schmiedebergs Arch. Pharmacol.
    Reist et al., 2004, Inter-relationships of intermediate phenotypes for serotonin function, impulsivity, and a 5-HT2A candidate allele: His452Tyr., Mol. Psychiatry
    McDonald et al., 2003, Enhancement of latent inhibition by two 5-HT2A receptor antagonists only when given at both pre-exposure and conditioning., Psychopharmacology (Berl.)
    Heiser et al., 2004, Effects of clozapine and its metabolites on the 5-HT2 receptor system in cortical and hippocampal cells in vitro., Prog. Neuropsychopharmacol. Biol. Psychiatry
    Broderick et al., 2004, Clozapine and cocaine effects on dopamine and serotonin release in nucleus accumbens during psychostimulant behavior and withdrawal., Prog. Neuropsychopharmacol. Biol. Psychiatry
    Travis et al., 1998, 5-HT2A receptor blockade in patients with schizophrenia treated with risperidone or clozapine. A SPET study using the novel 5-HT2A ligand 123I-5-I-R-91150., Br J Psychiatry
    Arranz et al., 1996, Analysis of a structural polymorphism in the 5-HT2A receptor and clinical response to clozapine., Neurosci. Lett.
    Salloum NC et al., 2014, Towards the clinical implementation of pharmacogenetics in bipolar disorder., BMC Med
    Friedman, 2013, Pimavanserin for the treatment of Parkinson's disease psychosis., Expert Opin Pharmacother
    Stark et al., 2007, Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT 2A receptors: functional receptor-binding and in vivo electrophysiological studies., Psychopharmacology (Berl.)
    Bortolozzi et al., 2007, In vivo actions of aripiprazole on serotonergic and dopaminergic systems in rodent brain., Psychopharmacology (Berl.)
    Meltzer et al., 2003, Serotonin receptors: their key role in drugs to treat schizophrenia., Prog. Neuropsychopharmacol. Biol. Psychiatry
    de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
    Anttila et al., 2001, A review of the pharmacological and clinical profile of mirtazapine., CNS Drug Rev
    Westenberg, 1999, Pharmacology of antidepressants: selectivity or multiplicity?, J Clin Psychiatry
    Gorman, 1999, Mirtazapine: clinical overview., J Clin Psychiatry
    Laakmann et al., 1999, Effects of mirtazapine on growth hormone, prolactin, and cortisol secretion in healthy male subjects., Psychoneuroendocrinology
    Waldinger et al., 2000, Treatment of hot flushes with mirtazapine: four case reports., Maturitas
    Nutt, 1999, Care of depressed patients with anxiety symptoms., J Clin Psychiatry
    Celada P et al., 2004, The therapeutic role of 5-HT1A and 5-HT2A receptors in depression., J Psychiatry Neurosci
    Pawlyk AC et al., 2006, Effects of the 5-HT2A antagonist mirtazapine in rat models of thermoregulation., Brain Res
    Deeks ED et al., 2010, Blonanserin: a review of its use in the management of schizophrenia., CNS Drugs
    Cohen, Risperidone., Pharmacotherapy
    Megens et al., 1994, Survey on the pharmacodynamics of the new antipsychotic risperidone., Psychopharmacology (Berl.)
    He et al., 1995, A pharmacological, pharmacokinetic and clinical overview of risperidone, a new antipsychotic that blocks serotonin 5-HT2 and dopamine D2 receptors., Int Clin Psychopharmacol
    Yamada et al., 2002, Prediction and assessment of extrapyramidal side effects induced by risperidone based on dopamine D(2) receptor occupancy., Synapse
    Muntasir HA et al., 2006, Inverse agonist activity of sarpogrelate, a selective 5-HT2A-receptor antagonist, at the constitutively active human 5-HT2A receptor., J Pharmacol Sci
    Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
    Eckler et al., 2003, Nefazodone in the rat: mimicry and antagonism of [-]-DOM-induced stimulus control., Pharmacol. Biochem. Behav.
    Hidalgo et al., 1999, Nefazodone in post-traumatic stress disorder: results from six open-label trials., Int Clin Psychopharmacol
    Davis et al., 1997, Nefazodone. A review of its pharmacology and clinical efficacy in the management of major depression., Drugs
    Avila et al., 2003, Does nefazodone improve both depression and Parkinson disease? A pilot randomized trial., J Clin Psychopharmacol
    Horton et al., 1999, Akinetopsia from nefazodone toxicity., Am. J. Ophthalmol.
    Taylor et al., 1995, Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug., J Clin Psychiatry
    Meyer et al., 1999, The effects of single dose nefazodone and paroxetine upon 5-HT2A binding potential in humans using [18F]-setoperone PET., Psychopharmacology (Berl.)
    Keks et al., 1999, Risperidone (Risperdal): clinical experience with a new antipsychosis drug., Expert Opin Investig Drugs
    Uchida et al., 2007, Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine., Life Sci.
    Fenton et al., 2005, Risperidone: a review of its use in the treatment of bipolar mania., CNS Drugs
    Maffioletti E et al., 2020, Association study between HTR2A rs6313 polymorphism and early response to risperidone and olanzapine in schizophrenia patients., Drug Dev Res
    López-Rodríguez R et al., 2013, Pharmacodynamic genetic variants related to antipsychotic adverse reactions in healthy volunteers., Pharmacogenomics
    Correia CT et al., 2010, Pharmacogenetics of risperidone therapy in autism: association analysis of eight candidate genes with drug efficacy and adverse drug reactions., Pharmacogenomics J
    Angelucci F et al., 2009, Delusion symptoms and response to antipsychotic treatment are associated with the 5-HT2A receptor polymorphism (102T/C) in Alzheimer's disease: a 3-year follow-up longitudinal study., J Alzheimers Dis
    Corena-McLeod M, 2015, Comparative Pharmacology of Risperidone and Paliperidone., Drugs R D
    Laika B et al., 2010, Pharmacogenetics and olanzapine treatment: CYP1A2*1F and serotonergic polymorphisms influence therapeutic outcome., Pharmacogenomics J
    Ujike H et al., 2008, Multiple genetic factors in olanzapine-induced weight gain in schizophrenia patients: a cohort study., J Clin Psychiatry
    Thomas P et al., 2008, Correlates of response to Olanzapine in a North Indian Schizophrenia sample., Psychiatry Res
    Moresco et al., 2004, Cerebral D2 and 5-HT2 receptor occupancy in Schizophrenic patients treated with olanzapine or clozapine., J. Psychopharmacol. (Oxford)
    Bymaster et al., 1999, Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro., Schizophr. Res.
    Padín et al., 2006, Parallel regulation by olanzapine of the patterns of expression of 5-HT2A and D3 receptors in rat central nervous system and blood cells., Neuropharmacology
    Sharpley et al., 2005, Olanzapine increases slow wave sleep and sleep continuity in SSRI-resistant depressed patients., J Clin Psychiatry
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
    Aly SA et al., 2009, Assessment of binding affinity to 5-hydroxytryptamine 2A (5-HT2A) receptor and inverse agonist activity of naftidrofuryl: comparison with those of sarpogrelate., J Pharmacol Sci
    Govitrapong et al., 2002, Platelet serotonin transporter in schizophrenic patients with and without neuroleptic treatment., Neurochem. Int.
    Govitrapong et al., 2000, Platelet 5-HT(2A) receptors in schizophrenic patients with and without neuroleptic treatment., Psychiatry Res
    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
    Kim DH et al., 2009, Building a better antipsychotic: receptor targets for the treatment of multiple symptom dimensions of schizophrenia., Neurotherapeutics
    Castilho et al., 1999, Antinociception elicited by aversive stimulation of the inferior colliculus., Pharmacol. Biochem. Behav.
    Shaw et al., 2000, Role of the 5-HT(2A)receptor and alpha(1)-adrenoceptor in the contractile response of rat pulmonary artery to 5-HT in the presence and absence of nitric oxide., Pulm Pharmacol Ther
    Connor et al., 2001, Second messengers in platelet aggregation evoked by serotonin and A23187, a calcium ionophore., Life Sci.
    Geerts et al., 1999, Involvement of 5-HT1B receptors in collar-induced hypersensitivity to 5-hydroxytryptamine of the rabbit carotid artery., Br. J. Pharmacol.
    Prins et al., 2001, Characterization of the receptors involved in the 5-HT-induced excitation of canine antral longitudinal muscle., Br. J. Pharmacol.
    Nabeshima et al., 1989, Effect of minaprine on cycloheximide-induced amnesia in mice., Eur. J. Pharmacol.
    Muramatsu et al., 1988, 5-HT2 antagonists and minaprine block the 5-HT-induced inhibition of dopamine release from rat brain striatal slices., Eur. J. Pharmacol.
    Kodama et al., 1992, Protective effect of minaprine against the abnormal changes of 2-deoxyglucose uptake by rat hippocampal slices induced by hypoxia/hypoglycemia., Jpn. J. Pharmacol.
    Bizière et al., 1985, Minaprine, a new drug with antidepressant properties., Drugs Exp Clin Res
    George et al., 2013, Newer antipsychotics and upcoming molecules for schizophrenia., Eur. J. Clin. Pharmacol.
    Uher R et al., 2009, Genetic predictors of response to antidepressants in the GENDEP project., Pharmacogenomics J
    Sanchez C et al., 2014, A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike?, Int Clin Psychopharmacol
    Li et al., 2003, A comparison of the effects of loxapine with ziprasidone and thioridazine on the release of dopamine and acetylcholine in the prefrontal cortex and nucleus accumbens., Psychopharmacology (Berl.)
    Adolph O et al., 2012, Promethazine inhibits NMDA-induced currents - new pharmacological aspects of an old drug., Neuropharmacology
    Sharma A et al., 2003, Classic histamine H1 receptor antagonists: a critical review of their metabolic and pharmacokinetic fate from a bird's eye view., Curr Drug Metab
    POWE CE et al., 1962, Propiomazine hydrochloride in obstetrical analgesia. A controlled study of 520 patients., JAMA
    Tiwari AK et al., 2013, Analysis of 34 candidate genes in bupropion and placebo remission., Int J Neuropsychopharmacol
    Mansbach et al., Blockade of drug-induced deficits in prepulse inhibition of acoustic startle by ziprasidone., Pharmacol. Biochem. Behav.
    Stahl et al., 2003, The psychopharmacology of ziprasidone: receptor-binding properties and real-world psychiatric practice., J Clin Psychiatry
    Kast et al., 2007, Treatment schedules for 5-HT2A blocking in progressive multifocal leukoencephalopathy using risperidone or ziprasidone., Bone Marrow Transplant.
    Ichikawa et al., 2002, Atypical antipsychotic drugs, quetiapine, iloperidone, and melperone, preferentially increase dopamine and acetylcholine release in rat medial prefrontal cortex: role of 5-HT1A receptor agonism., Brain Res.
    Lu et al., 2002, A case of ziprasidone-induced mania and the role of 5-HT2A in mood changes induced by atypical antipsychotics., J Clin Psychiatry
    Mamo et al., 2004, A PET study of dopamine D2 and serotonin 5-HT2 receptor occupancy in patients with schizophrenia treated with therapeutic doses of ziprasidone., Am J Psychiatry
    Rashid et al., 2002, Effects of sarpogrelate, a novel 5-HT2 antagonist, on 5-HT-induced endothelium-dependent relaxations in porcine coronary artery., Jpn. J. Pharmacol.
    Hoenicke et al., 1992, The discriminative stimulus effects of clozapine in pigeons: involvement of 5-hydroxytryptamine1C and 5-hydroxytryptamine2 receptors., J. Pharmacol. Exp. Ther.
    Callaway et al., 1992, Serotonin 5-HT1-like receptors mediate hyperactivity in rats induced by 3,4-methylenedioxymethamphetamine., Neuropsychopharmacology
    Calka et al., Effect of cyproheptadine on serum leptin levels., Adv Ther
    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.
    Sánchez Martín A et al., 2013, Impact of pharmacogenetics on CNS side effects related to efavirenz., Pharmacogenomics
    Conn et al., 1987, Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors., J. Pharmacol. Exp. Ther.
    Marek et al., 1992, A comparison of trazodone and fluoxetine: implications for a serotonergic mechanism of antidepressant action., Psychopharmacology (Berl.)
    Pazzagli et al., 1999, Trazodone increases extracellular serotonin levels in the frontal cortex of rats., Eur. J. Pharmacol.
    Marcoli et al., 2001, Inhibitory presynaptic 5-hydroxytryptamine(2A) receptors regulate evoked glutamate release from rat cerebellar mossy fibers., J. Pharmacol. Exp. Ther.
    Luparini et al., 2004, A cortical GABA-5HT interaction in the mechanism of action of the antidepressant trazodone., Prog. Neuropsychopharmacol. Biol. Psychiatry
    Stryjer R et al., 2003, Treatment of neuroleptic-induced akathisia with the 5-HT2A antagonist trazodone., Clin Neuropharmacol
    Balsara JJ et al., 2005, Effects of the antidepressant trazodone, a 5-HT 2A/2C receptor antagonist, on dopamine-dependent behaviors in rats., Psychopharmacology (Berl)
    Cargnin S et al., 2014, Combined effect of common gene variants on response to drug withdrawal therapy in medication overuse headache., Eur J Clin Pharmacol
    Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr
    Maj et al., 1977, Doxepin as a blocker of central serotonin receptors., Pharmakopsychiatr Neuropsychopharmakol
    Lohoff FW et al., 2013, Serotonin receptor 2A (HTR2A) gene polymorphism predicts treatment response to venlafaxine XR in generalized anxiety disorder., Pharmacogenomics J
    Demirbugen Oz M et al., 2018, The relationship between the serotonin 2A receptor gene -1438A/G and 102T/C polymorphisms and citalopram/sertraline-induced nausea in major depressed patients., Hum Psychopharmacol
    Smith RM et al., 2013, Multiple regulatory variants modulate expression of 5-hydroxytryptamine 2A receptors in human cortex., Biol Psychiatry
    Illi A et al., 2009, 5-HTR1A, 5-HTR2A, 5-HTR6, TPH1 and TPH2 polymorphisms and major depression., Neuroreport
    Paddock S et al., 2007, Association of GRIK4 with outcome of antidepressant treatment in the STAR*D cohort., Am J Psychiatry
    Pandey DK et al., 2010, A novel 5-HT(2A) receptor antagonist exhibits antidepressant-like effects in a battery of rodent behavioural assays: approaching early-onset antidepressants., Pharmacol Biochem Behav
    Kato M et al., 2006, Effects of the serotonin type 2A, 3A and 3B receptor and the serotonin transporter genes on paroxetine and fluvoxamine efficacy and adverse drug reactions in depressed Japanese patients., Neuropsychobiology
    Suzuki Y et al., 2006, Polymorphisms in the 5-hydroxytryptamine 2A receptor and CytochromeP4502D6 genes synergistically predict fluvoxamine-induced side effects in japanese depressed patients., Neuropsychopharmacology
  • PIMAVANSERIN   HTR2A

    Interaction Score: 1.84

    Interaction Types & Directionality:
    inverse agonist (inhibitory)
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name Pimavanserin

    PMIDs:
    24016069


    Sources:
    TdgClinicalTrial TTD

  • VOLINANSERIN   HTR2A

    Interaction Score: 1.22

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name volinanserin
    Novel drug target Established target
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • NELOTANSERIN   HTR2A

    Interaction Score: 1.22

    Interaction Types & Directionality:
    inverse agonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor inverse agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions TTD

  • TEMANOGREL   HTR2A

    Interaction Score: 1.22

    Interaction Types & Directionality:
    inverse agonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor inverse agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions TTD

  • PRUVANSERIN   HTR2A

    Interaction Score: 1.22

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions TTD

  • IFERANSERIN   HTR2A

    Interaction Score: 1.22

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name iferanserin ointment
    Novel drug target Established target
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • CYPROHEPTADINE   HTR2A

    Interaction Score: 1.07

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    12233819 1403790 1358088 16418149 12498911


    Sources:
    TdgClinicalTrial TEND

  • SARPOGRELATE   HTR2A

    Interaction Score: 0.92

    Interaction Types & Directionality:
    inverse agonist (inhibitory)
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    19672037 17031071


    Sources:
    TTD

  • MESORIDAZINE   HTR2A

    Interaction Score: 0.77

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    15357957 11561066 10991983


    Sources:
    TdgClinicalTrial TEND

  • CYCLOBENZAPRINE   HTR2A

    Interaction Score: 0.73

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    8884233 12498911 21975349


    Sources:
    TdgClinicalTrial TEND TTD

  • EPLIVANSERIN   HTR2A

    Interaction Score: 0.61

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PIMAVANSERIN TARTRATE   HTR2A

    Interaction Score: 0.61

    Interaction Types & Directionality:
    inverse agonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor inverse agonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MINAPRINE   HTR2A

    Interaction Score: 0.61

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    2530096 2975224 1361012 3836113


    Sources:
    TdgClinicalTrial TEND

  • NEFAZODONE   HTR2A

    Interaction Score: 0.61

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    7855217 12873632 10220119 9098663 14520130 10577608 7649970 10435395


    Sources:
    TdgClinicalTrial TEND

  • PALIPERIDONE   HTR2A

    Interaction Score: 0.61

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name paliperidone ER, paliperidone palmitate
    Novel drug target Established target
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    7520908 7524043 7531353 7542676 11132243 12211096


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • BLONANSERIN   HTR2A

    Interaction Score: 0.61

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    20030420


    Sources:
    TTD

  • NEMIFITIDE   HTR2A

    Interaction Score: 0.61

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name INN-00835, nemifitide
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • ZOTEPINE   HTR2A

    Interaction Score: 0.61

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LUMATEPERONE   HTR2A

    Interaction Score: 0.49

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name ITI-007, ITI-722
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    30596390


    Sources:
    TdgClinicalTrial ChemblInteractions TTD

  • TRAZODONE   HTR2A

    Interaction Score: 0.47

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name trazodone extended release, DDS-04A,Oleptro

    PMIDs:
    3039120 1365657 10594316 11714900 15610924 7855217 12782915 15614572


    Sources:
    TdgClinicalTrial TEND

  • THIOTHIXENE   HTR2A

    Interaction Score: 0.46

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    10821438 8593484


    Sources:
    ChemblInteractions

  • CHLORPROTHIXENE   HTR2A

    Interaction Score: 0.44

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    3774629 2891550


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • METHYSERGIDE   HTR2A

    Interaction Score: 0.43

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10080233 11061982 11720080 10455282 11704657


    Sources:
    TdgClinicalTrial TEND

  • ESMIRTAZAPINE   HTR2A

    Interaction Score: 0.41

    Interaction Types & Directionality:
    inverse agonist (inhibitory)

    Interaction Info:
    Trial Name esmirtazapine, ORG-4420
    Novel drug target Established target

    PMIDs:
    26047892


    Sources:
    TdgClinicalTrial

  • TRELANSERIN   HTR2A

    Interaction Score: 0.41

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes
    Trial Name trelanserin, SL 65.0472

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • OCAPERIDONE   HTR2A

    Interaction Score: 0.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    TTD

  • MIDOMAFETAMINE   HTR2A

    Interaction Score: 0.37

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    7824160 2871581


    Sources:
    TTD

  • BREXPIPRAZOLE   HTR2A

    Interaction Score: 0.37

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes
    Trial Name OPC-34712

    PMIDs:
    24947465


    Sources:
    TdgClinicalTrial ChemblInteractions

  • ARIPIPRAZOLE   HTR2A

    Interaction Score: 0.36

    Interaction Types & Directionality:
    partial agonist (activating)
    agonist (activating)
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Trial Name Abilify

    PMIDs:
    17242925 17265076 14642974 26346901


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • MIRTAZAPINE   HTR2A

    Interaction Score: 0.35

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes
    Trial Name mirtazapine,Remeron, Remeron SolTab, Reflex

    PMIDs:
    11607047 10446734 10446735 10451911 11063897 10446738 15309042 17067560


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • PROPIOMAZINE   HTR2A

    Interaction Score: 0.35

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    17016423 17139284 19110200 22507664 12678691 14488364


    Sources:
    TdgClinicalTrial TEND

  • FLIBANSERIN   HTR2A

    Interaction Score: 0.34

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Flibanserin
    Novel drug target Established target

    PMIDs:
    26412054 12177684 12890707


    Sources:
    TdgClinicalTrial TTD

  • THIORIDAZINE   HTR2A

    Interaction Score: 0.33

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes
    Trial Name -

    PMIDs:
    7898773 8680734 9918563 2866233 2423886


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • ROLUPERIDONE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • MOLINDONE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ASENAPINE MALEATE   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ABAPERIDONE   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ZIPRASIDONE   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name ziprasidone HCl, ziprasidone mesylate,Geodon, Zeldox
    Novel drug target Established target

    PMIDs:
    11509214 14728084 17450180 12445705 17848919 12530423 15121646


    Sources:
    TdgClinicalTrial TEND

  • LOXAPINE   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name AZ-004
    Novel drug target Established target
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    12664192


    Sources:
    TdgClinicalTrial ChemblInteractions

  • MESORIDAZINE BESYLATE   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LURASIDONE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RISPERDAL   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name Risperdal
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • TERGURIDE   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name terguride
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • SB-773812   HTR2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SERTINDOLE   HTR2A

    Interaction Score: 0.28

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Serdolect
    Novel drug target Established target

    PMIDs:
    11594443 7530204 16925508


    Sources:
    TdgClinicalTrial TEND

  • PROMAZINE   HTR2A

    Interaction Score: 0.25

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    12106771 10980325 17016423 17139284 19110200


    Sources:
    TdgClinicalTrial TEND

  • LURASIDONE   HTR2A

    Interaction Score: 0.24

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name lurasidone, SM-13496,Latuda
    Novel drug target Established target

    PMIDs:
    23545936


    Sources:
    TdgClinicalTrial

  • ANIRACETAM   HTR2A

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11412837


    Sources:
    TTD

  • KETANSERIN   HTR2A

    Interaction Score: 0.23

    Interaction Types & Directionality:
    inverse agonist (inhibitory)
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    9767524 17031071


    Sources:
    NCI

  • PAROXETINE   HTR2A

    Interaction Score: 0.23

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    11403977 11136637 19361869 18253134 17697394 14514498 23338224 5821956


    Sources:
    PharmGKB

  • QUETIAPINE FUMARATE   HTR2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ZIPRASIDONE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • FLUVOXAMINE   HTR2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19361869 16874005 16205777


    Sources:
    PharmGKB

  • ZIPRASIDONE MESYLATE   HTR2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ARIPIPRAZOLE LAUROXIL   HTR2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • VABICASERIN HYDROCHLORIDE   HTR2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • THIOTHIXENE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CARPHENAZINE MALEATE   HTR2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ILOPERIDONE   HTR2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Novel drug target Established target

    PMIDs:
    8997630 12861482


    Sources:
    TdgClinicalTrial ChemblInteractions TTD

  • MIANSERIN   HTR2A

    Interaction Score: 0.18

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11004734


    Sources:
    TdgClinicalTrial TEND

  • OLANZAPINE   HTR2A

    Interaction Score: 0.18

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv
    Novel drug target Established target
    Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

    PMIDs:
    32462699 24885933 19636338 19494443 19193342 19000940 15358979 16038601 17316700 10227113 14530903 16905159 15816787 11752352 17848919 25032030


    Sources:
    TdgClinicalTrial ChemblInteractions TEND PharmGKB

  • QUETIAPINE   HTR2A

    Interaction Score: 0.16

    Interaction Types & Directionality:
    agonist (activating)
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Seroquel
    Novel drug target Established target

    PMIDs:
    17563257 11132243 12973385 17848919 16038601


    Sources:
    TdgClinicalTrial TEND

  • HALOPERIDOL LACTATE   HTR2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ZICRONAPINE   HTR2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • HALOPERIDOL DECANOATE   HTR2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CLOZAPINE   HTR2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    7520908 12973385 15037867 14530903 14751426 14687870 9926100 8916101 24885933


    Sources:
    TdgClinicalTrial ChemblInteractions NCI TEND PharmGKB

  • RISPERIDONE   HTR2A

    Interaction Score: 0.14

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    11132243 15992090 17316700 15907153 32462699 23859574 19997080 19494443 25943458


    Sources:
    TdgClinicalTrial ChemblInteractions TEND PharmGKB

  • AMITRIPTYLINE   HTR2A

    Interaction Score: 0.14

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name OMS-103HP
    Novel drug target Established target

    PMIDs:
    7855217 19800913


    Sources:
    TdgClinicalTrial

  • DOXEPIN   HTR2A

    Interaction Score: 0.14

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target

    PMIDs:
    7855217 19179941 309138


    Sources:
    TdgClinicalTrial

  • ONDANSETRON   HTR2A

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9767524


    Sources:
    NCI

  • ASENAPINE   HTR2A

    Interaction Score: 0.14

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Asenapine
    Novel drug target Established target

    PMIDs:
    18308814 10592235 21655346


    Sources:
    TdgClinicalTrial

  • OLANZAPINE PAMOATE   HTR2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TRYPTAMINE   HTR2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LOXAPINE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CYCLOBENZAPRINE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RENZAPRIDE   HTR2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Established target
    Trial Name renzapride

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • TRAZODONE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHLORPROMAZINE   HTR2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    binder
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    7908055 10821438 8593484


    Sources:
    ChemblInteractions

  • THIETHYLPERAZINE   HTR2A

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TEND

  • NEFAZODONE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LOXAPINE SUCCINATE   HTR2A

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ESMIRTAZAPINE MALEATE   HTR2A

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BIFEPRUNOX   HTR2A

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name bifeprunox, DU127090
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • DROPERIDOL   HTR2A

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ESCITALOPRAM   HTR2A

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    19365399 24424469


    Sources:
    PharmGKB

  • CITALOPRAM   HTR2A

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30221791 23158458 19590397 17671280


    Sources:
    PharmGKB

  • SUMATRIPTAN   HTR2A

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25096645


    Sources:
    PharmGKB

  • TRIMIPRAMINE MALEATE   HTR2A

    Interaction Score: 0.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • VENLAFAXINE   HTR2A

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22006095


    Sources:
    PharmGKB

  • PROMAZINE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.08

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BUPROPION   HTR2A

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22947179


    Sources:
    PharmGKB

  • EFAVIRENZ   HTR2A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23859571


    Sources:
    PharmGKB

  • TRIFLUOPERAZINE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TEDATIOXETINE   HTR2A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • THIORIDAZINE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHLORPROMAZINE HYDROCHLORIDE   HTR2A

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • HALOPERIDOL   HTR2A

    Interaction Score: 0.03

    Interaction Types & Directionality:
    other/unknown
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    7520908 12629531


    Sources:
    ChemblInteractions

  • PROCHLORPERAZINE   HTR2A

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TEND

  • LITHIUM   HTR2A

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10758249


    Sources:
    NCI

  • PIMOZIDE   HTR2A

    Interaction Score: 0.02

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • FLUOXETINE   HTR2A

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name NPL-2008, Fluoxetine
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • Ensembl: ENSG00000102468

    • Version: 101_38

    Alternate Names:
    HTR2A Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TEND: P28223

    • Version: 01-August-2011

    Alternate Names:
    P28223 Uniprot Accession
    5HT2A_HUMAN Uniprot Id
    HTR2A Gene Symbol

    Gene Info:
    Target Main Class Receptors
    Target Subclass Rhodopsin
    Transmembrane Helix Count 7

    Publications:

  • RussLampel: ENSG00000102468

    • Version: 26-July-2011

    Alternate Names:
    HTR2A Display Id
    5-HYDROXYTRYPTAMINE 2A RECEPTOR (5-HT-2A) (SEROTONIN RECEPTOR 2A) (5- HT-2). [SOURCE:UNIPROT/SWISSPROT;ACC:P28223] Description
    ENSG00000102468 Ensembl Gene Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • HopkinsGroom: P28223

    • Version: 11-September-2012

    Alternate Names:
    3356 Entrez Gene Id
    5-HYDROXYTRYPTAMINE RECEPTOR 2A Uniprot Protein Name
    HTR2A Uniprot Gene Name

    Gene Info:
    Human Readable Name G PROTEIN COUPLED RECEPTOR
    Interpro Acc IPR000276
    Uniprot Status Swiss-Prot

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: P28223

    • Version: January-2014

    Alternate Names:
    HTR2A Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass GPCR
    Target Subclass Rhodopsin

    Publications:

  • PharmGKB: HTR2A

    • Version: 18-August-2020

    Alternate Names:
    PA193 PharmGKB ID

    Gene Info:

    Publications:
    Tiwari AK et al., 2013, Analysis of 34 candidate genes in bupropion and placebo remission., Int J Neuropsychopharmacol
    Ujike H et al., 2008, Multiple genetic factors in olanzapine-induced weight gain in schizophrenia patients: a cohort study., J Clin Psychiatry
    Angelucci F et al., 2009, Delusion symptoms and response to antipsychotic treatment are associated with the 5-HT2A receptor polymorphism (102T/C) in Alzheimer's disease: a 3-year follow-up longitudinal study., J Alzheimers Dis

  • TTD: 5-HT 2A receptor

    • Version: 2020.06.01

    Alternate Names:
    HTR2A TTD Gene Abbreviation
    T32060 TTD Target ID

    Gene Info:

    Publications:
    Guo JD et al., 2009, Bi-directional modulation of bed nucleus of stria terminalis neurons by 5-HT: molecular expression and functional properties of excitatory 5-HT receptor subtypes., Neuroscience
    Chen J et al., 2011, Novel ocular antihypertensive compounds in clinical trials., Clin Ophthalmol

  • NCI: HTR2A

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Serretti et al., Serotonin receptor 2A, 2C, 1A genes and response to lithium prophylaxis in mood disorders., J Psychiatr Res
    Kasho et al., 1998, Serotonin enhances the production of type IV collagen by human mesangial cells., Kidney Int.
    Arranz et al., 1996, Analysis of a structural polymorphism in the 5-HT2A receptor and clinical response to clozapine., Neurosci. Lett.

  • HingoraniCasas: ENSG00000102468

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000102468 Gene Symbol
    HTR2A Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • ChemblInteractions: HTR2

    • Version: chembl_23

    Alternate Names:
    HTR2 GENE_SYMBOL
    HTR2A GENE_SYMBOL
    5-hydroxytryptamine receptor 2A UNIPROT

    Gene Info:

    Publications:

  • dGene: HTR2A

    • Version: 27-Jun-2013

    Alternate Names:
    3356 Gene ID
    5-HT2A dGene Synonym
    HTR2 dGene Synonym

    Gene Info:

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    Publications:

  • Pharos: HTR2A

    • Version: 01-February-2022

    Alternate Names:
    5-hydroxytryptamine receptor 2A Gene Name
    P28223 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21