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HTR1A Gene Record

  • Summary
  • Interactions
  • Claims
  • HTR1A 3350 Druggable Genome

    Alternate Names:

    3350
    5-HYDROXYTRYPTAMINE RECEPTOR 1A
    HTR1A
    5-HT-1A
    5-HT1A
    5HT1a
    ADRB2RL1
    ADRBRL1
    G-21
    PFMCD
    109760
    5286
    ENSG00000178394
    OTTHUMG00000162279
    Serotonin receptor 1A
    P08908
    5HT1A_HUMAN
    PA192
    5-HYDROXYTRYPTAMINE 1A RECEPTOR (5-HT-1A) (SEROTONIN RECEPTOR 1A) (5- HT1A) (G-21). [SOURCE:UNIPROT/SWISSPROT;ACC:P08908]
    5-HT 1A receptor
    T78709

    Gene Info:

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

    Gene Categories: Category Details

    CELL SURFACE
    G PROTEIN COUPLED RECEPTOR
    DRUGGABLE GENOME

    Publications:

    Bobo, 2013, Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults., Expert Rev Clin Pharmacol
    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.
    Marona-Lewicka et al., 2004, Aripiprazole (OPC-14597) fully substitutes for the 5-HT1A receptor agonist LY293284 in the drug discrimination assay in rats., Psychopharmacology (Berl.)
    Cosi et al., 2005, Clozapine, ziprasidone and aripiprazole but not haloperidol protect against kainic acid-induced lesion of the striatum in mice, in vivo: role of 5-HT1A receptor activation., Brain Res.
    Jordan et al., 2002, The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor., Eur. J. Pharmacol.
    Jordan et al., 2004, In vivo effects of aripiprazole on cortical and striatal dopaminergic and serotonergic function., Eur. J. Pharmacol.
    Swainston Harrison et al., 2004, Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder., Drugs
    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
    Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
    Odagaki et al., 2005, Trazodone and its active metabolite m-chlorophenylpiperazine as partial agonists at 5-HT1A receptors assessed by [35S]GTPgammaS binding., J. Psychopharmacol. (Oxford)
    Subhash et al., 2002, Alterations in 5-HT(1A) receptors and adenylyl cyclase response by trazodone in regions of rat brain., Life Sci.
    Sultan MA et al., 2017, Adjunctive Trazodone and Depression Outcome in Adolescents Treated with Serotonin Re-uptake Inhibitors., J Can Acad Child Adolesc Psychiatry
    Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Maeda et al., 2014, Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator., J. Pharmacol. Exp. Ther.
    Crisafulli C et al., 2012, Case-control association study for 10 genes in patients with schizophrenia: influence of 5HTR1A variation rs10042486 on schizophrenia and response to antipsychotics., Eur Arch Psychiatry Clin Neurosci
    Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
    Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
    Pranzatelli et al., 1991, Characterization of 5-hydroxytryptamine 1A-like binding sites in human ganglioneuroblastoma., Neurosci. Lett.
    Sugimoto et al., 2003, The tricyclic antidepressant clomipramine increases plasma glucose levels of mice., J. Pharmacol. Sci.
    Scrogin et al., 2000, Methysergide delays the decompensatory responses to severe hemorrhage by activating 5-HT(1A) receptors., Am. J. Physiol. Regul. Integr. Comp. Physiol.
    Skyba et al., 2003, Joint manipulation reduces hyperalgesia by activation of monoamine receptors but not opioid or GABA receptors in the spinal cord., Pain
    Sugimoto et al., 2003, Involvement of 5-HT(2) receptor in imipramine-induced hyperglycemia in mice., Horm. Metab. Res.
    Johnson et al., 2001, Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain., Eur. J. Pharmacol.
    Adamec et al., 2004, Effects of systemic injections of vilazodone, a selective serotonin reuptake inhibitor and serotonin 1A receptor agonist, on anxiety induced by predator stress in rats., Eur. J. Pharmacol.
    Page et al., 2002, Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist., J. Pharmacol. Exp. Ther.
    Auclair et al., 2007, Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors disrupt basal PPI of the startle reflex in rats., Psychopharmacology (Berl.)
    Bardin et al., 2006, Antipsychotic-like vs cataleptogenic actions in mice of novel antipsychotics having D2 antagonist and 5-HT1A agonist properties., Neuropsychopharmacology
    Newman-Tancredi et al., 2007, Neuropharmacological profile of bifeprunox: merits and limitations in comparison with other third-generation antipsychotics., Curr Opin Investig Drugs
    Newman-Tancredi A et al., 2005, Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia., Int J Neuropsychopharmacol
    Johnston TH et al., 2004, Drugs in development for Parkinson's disease., Curr Opin Investig Drugs
    Tfelt-Hansen et al., 2000, Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy., Drugs
    Boers et al., 2004, Naratriptan has a selective inhibitory effect on trigeminovascular neurones at central 5-HT1A and 5-HT(1B/1D) receptors in the cat: implications for migraine therapy., Cephalalgia
    George et al., 2013, Newer antipsychotics and upcoming molecules for schizophrenia., Eur. J. Clin. Pharmacol.
    Yoshikawa A et al., 2020, A functional HTR1A polymorphism, rs6295, predicts short-term response to lurasidone: confirmation with meta-analysis of other antipsychotic drugs., Pharmacogenomics J
    Kato M et al., 2009, Effect of 5-HT1A gene polymorphisms on antidepressant response in major depressive disorder., Am J Med Genet B Neuropsychiatr Genet
    Bosia M et al., 2015, COMT Val158Met and 5-HT1A-R -1019 C/G polymorphisms: effects on the negative symptom response to clozapine., Pharmacogenomics
    Chou et al., 2003, Occupancy of 5-HT1A receptors by clozapine in the primate brain: a PET study., Psychopharmacology (Berl.)
    Newman-Tancredi et al., 2003, Comparison of hippocampal G protein activation by 5-HT(1A) receptor agonists and the atypical antipsychotics clozapine and S16924., Naunyn Schmiedebergs Arch. Pharmacol.
    Tomić et al., 2004, Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential., Bioorg. Med. Chem. Lett.
    Zahorodna et al., 2004, The influence of repeated administration of clozapine and haloperidol on the effects of the activation of 5-HT(1A), 5-HT(2) and 5-HT(4) receptors in rat frontal cortex., J. Physiol. Pharmacol.
    Hagino et al., 2002, Effects of clozapine on the efflux of serotonin and dopamine in the rat brain: the role of 5-HT1A receptors., Can. J. Physiol. Pharmacol.
    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.
    Wood et al., 2006, Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade., CNS Neurol Disord Drug Targets
    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.
    Niitsu T et al., 2013, Pharmacogenetics in major depression: a comprehensive meta-analysis., Prog Neuropsychopharmacol Biol Psychiatry
    Ishiguro S et al., 2011, Determinants of pharmacodynamic trajectory of the therapeutic response to paroxetine in Japanese patients with panic disorder., Eur J Clin Pharmacol
    Yevtushenko OO et al., 2010, Early response to selective serotonin reuptake inhibitors in panic disorder is associated with a functional 5-HT1A receptor gene polymorphism., J Affect Disord
    Illi A et al., 2009, 5-HTR1A, 5-HTR2A, 5-HTR6, TPH1 and TPH2 polymorphisms and major depression., Neuroreport
    Baune BT et al., 2008, Serotonin receptor 1A-1019C/G variant: impact on antidepressant pharmacoresponse in melancholic depression?, Neurosci Lett
    Drago A et al., 2008, 5-HT1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies., Int J Neuropsychopharmacol
    Rehman et al., 1999, Modification of sexual behavior of Long-Evans male rats by drugs acting on the 5-HT1A receptor., Brain Res.
    Liang, 1999, Pre- or post-training injection of buspirone impaired retention in the inhibitory avoidance task: involvement of amygdala 5-HT1A receptors., Eur. J. Neurosci.
    Dupuis et al., 1999, Modulation of 5-HT1A receptor signalling by point-mutation of cysteine351 in the rat Galpha(o) protein., Neuropharmacology
    Osei-Owusu et al., 2004, Buspirone raises blood pressure through activation of sympathetic nervous system and by direct activation of alpha1-adrenergic receptors after severe hemorrhage., J. Pharmacol. Exp. Ther.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Becker et al., 1999, Prevention by 5-HT1A receptor agonists of restraint stress- and yohimbine-induced release of cholecystokinin in the frontal cortex of the freely moving rat., Neuropharmacology
    de Boer et al., 1999, Selective antiaggressive effects of alnespirone in resident-intruder test are mediated via 5-hydroxytryptamine1A receptors: A comparative pharmacological study with 8-hydroxy-2-dipropylaminotetralin, ipsapirone, buspirone, eltoprazine, and WAY-100635., J. Pharmacol. Exp. Ther.
    Kishi T et al., 2010, Serotonin 1A receptor gene is associated with Japanese methamphetamine-induced psychosis patients., Neuropharmacology
    de Paulis T, 2007, Drug evaluation: PRX-00023, a selective 5-HT1A receptor agonist for depression., Curr Opin Investig Drugs
    Iyer GR et al., 2007, Tolerability, pharmacokinetics, and neuroendocrine effects of PRX-00023, a novel 5-HT1A agonist, in healthy subjects., J Clin Pharmacol
    Rickels K et al., 2008, Effects of PRX-00023, a novel, selective serotonin 1A receptor agonist on measures of anxiety and depression in generalized anxiety disorder: results of a double-blind, placebo-controlled trial., J Clin Psychopharmacol
    Schmidt et al., 2001, Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile., Eur. J. Pharmacol.
    Wilner et al., 2002, The anxiolytic effect of the novel antipsychotic ziprasidone compared with diazepam in subjects anxious before dental surgery., J Clin Psychopharmacol
    Stahl et al., 2003, The psychopharmacology of ziprasidone: receptor-binding properties and real-world psychiatric practice., J Clin Psychiatry
    Rollema et al., 2000, 5-HT(1A) receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex., Biol. Psychiatry
    Sprouse et al., 1999, Comparison of the novel antipsychotic ziprasidone with clozapine and olanzapine: inhibition of dorsal raphe cell firing and the role of 5-HT1A receptor activation., Neuropsychopharmacology
    Cates ME, 2003, Ziprasidone--not an option for serotonin syndrome., CMAJ
    Akai et al., 1991, [Anxiolytic effects of lisuride and its agonistic action to central 5-HT1A receptors]., Nippon Yakurigaku Zasshi
    Cunningham et al., 1987, Discriminative stimulus properties of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OHDPAT): implications for understanding the actions of novel anxiolytics., Eur. J. Pharmacol.
    Kimura et al., 1991, Dual activation by lisuride of central serotonin 5-HT(1A) and dopamine D(2) receptor sites: drug discrimination and receptor binding studies., Behav Pharmacol
    Marona-Lewicka et al., 2002, Re-evaluation of lisuride pharmacology: 5-hydroxytryptamine1A receptor-mediated behavioral effects overlap its other properties in rats., Psychopharmacology (Berl.)
    Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem
    Miyazawa et al., 1991, [Effect of lisuride on experimental cerebral infarction in rats]., Nippon Yakurigaku Zasshi
    Scheller et al., 2009, The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease., Naunyn Schmiedebergs Arch. Pharmacol.
    Rubio-Beltrán E et al., 2018, Is selective 5-HT<sub>1F</sub> receptor agonism an entity apart from that of the triptans in antimigraine therapy?, Pharmacol Ther
    Martin, 1997, Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine., Cephalalgia
    Hillegaart V et al., 1998, Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5-HT1A and 5-HT1B receptor agonists 8-OH-DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD-299 and NAS-181., Br J Pharmacol
    Tordera R et al., 2003, Effect of different 5-HT1A receptor antagonists in combination with paroxetine on expression of the immediate-early gene Arc in rat brain., Neuropharmacology
    Bang-Andersen et al., 2011, Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder., J. Med. Chem.
    Kamei K et al., 2006, Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan., Bioorg Med Chem
    Riga MS et al., 2016, The serotonergic hallucinogen 5-methoxy-N,N-dimethyltryptamine disrupts cortical activity in a regionally-selective manner via 5-HT(1A) and 5-HT(2A) receptors., Neuropharmacology
    Hong CJ et al., 2006, Response to fluoxetine and serotonin 1A receptor (C-1019G) polymorphism in Taiwan Chinese major depressive disorder., Pharmacogenomics J
  • NALUZOTAN   HTR1A

    Interaction Score: 5.52

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name PRX-00023
    Novel drug target Established target
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist

    PMIDs:
    17263189 17495280 18344738


    Sources:
    TdgClinicalTrial ChemblInteractions

  • ROBALZOTAN   HTR1A

    Interaction Score: 3.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    9886765 12726821


    Sources:
    ChemblInteractions

  • OSEMOZOTAN   HTR1A

    Interaction Score: 3.31

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist
    Direct Interaction yes
    Trial Name MN-305

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions TTD

  • LISURIDE   HTR1A

    Interaction Score: 2.94

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    1678728 2887435 11224054 12373423 18691132 1783326


    Sources:
    TdgClinicalTrial TEND

  • GEPIRONE   HTR1A

    Interaction Score: 2.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name Gepirone
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD

  • XALIPRODEN   HTR1A

    Interaction Score: 2.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Established target
    Trial Name xaliproden, SR 57746A

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD

  • VILAZODONE   HTR1A

    Interaction Score: 2.21

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name vilazodone hydrochloride, SB 659746A
    Novel drug target Established target

    PMIDs:
    15507223 12183683


    Sources:
    TdgClinicalTrial TTD

  • SARIZOTAN   HTR1A

    Interaction Score: 1.66

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15707540 15298067


    Sources:
    TTD

  • BUSPIRONE   HTR1A

    Interaction Score: 1.58

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

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10064829 10215901 10428422 14769835 11752352 10221756 10027850


    Sources:
    TdgClinicalTrial TEND TTD

  • 5-MEO-DMT   HTR1A

    Interaction Score: 1.1

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    26477571


    Sources:
    DTC

  • PICLOZOTAN   HTR1A

    Interaction Score: 1.1

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BEFIRADOL   HTR1A

    Interaction Score: 1.1

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • XYLOMETAZOLINE HYDROCHLORIDE   HTR1A

    Interaction Score: 1.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LECOZOTAN HYDROCHLORIDE   HTR1A

    Interaction Score: 1.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ZALOSPIRONE   HTR1A

    Interaction Score: 1.1

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • BIFEPRUNOX   HTR1A

    Interaction Score: 0.92

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor partial agonist
    Direct Interaction yes
    Trial Name bifeprunox, DU127090

    PMIDs:
    17393144 16237379 17659474


    Sources:
    TdgClinicalTrial ChemblInteractions

  • ZOLMITRIPTAN   HTR1A

    Interaction Score: 0.88

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name zolmitriptan,Zomig
    Novel drug target Established target

    PMIDs:
    11513839 29352859 9399012


    Sources:
    TdgClinicalTrial

  • LURASIDONE   HTR1A

    Interaction Score: 0.88

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    23545936 31636356


    Sources:
    TdgClinicalTrial PharmGKB

  • BREXPIPRAZOLE   HTR1A

    Interaction Score: 0.88

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

    Interaction Info:
    Novel drug target Established target
    Trial Name OPC-34712
    Direct Interaction yes

    PMIDs:
    24947465


    Sources:
    TdgClinicalTrial ChemblInteractions TTD

  • NARATRIPTAN   HTR1A

    Interaction Score: 0.83

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name naratriptan,Naramig, Amerge
    Novel drug target Established target

    PMIDs:
    11152011 14728705


    Sources:
    TdgClinicalTrial

  • ARIPIPRAZOLE   HTR1A

    Interaction Score: 0.83

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

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor partial agonist
    Trial Name Abilify

    PMIDs:
    14647959 15862515 12063084 14709325 15257633 26346901


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • METHYSERGIDE   HTR1A

    Interaction Score: 0.77

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    1838579 14501155 11049861 14581123 14517765


    Sources:
    TdgClinicalTrial TEND

  • FLUVOXAMINE   HTR1A

    Interaction Score: 0.74

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23733030 21688171 19800133 19590397 18484082 18387740 18047755


    Sources:
    PharmGKB

  • ROTIGOTINE   HTR1A

    Interaction Score: 0.66

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    18704368 18691132


    Sources:
    TEND

  • FLIBANSERIN   HTR1A

    Interaction Score: 0.61

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name Flibanserin

    PMIDs:
    26412054 12177684 12890707


    Sources:
    TdgClinicalTrial TTD

  • TRAZODONE   HTR1A

    Interaction Score: 0.59

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

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

    PMIDs:
    7855217 15888508 12127910 29056986


    Sources:
    TdgClinicalTrial TEND TTD

  • VORTIOXETINE   HTR1A

    Interaction Score: 0.55

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name Lu AA21004
    Novel drug target Established target

    PMIDs:
    21486038 16290165


    Sources:
    TdgClinicalTrial

  • VILAZODONE HYDROCHLORIDE   HTR1A

    Interaction Score: 0.55

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor partial agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ZIPRASIDONE   HTR1A

    Interaction Score: 0.55

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    11513838 11910268 14728084 12923612 10924666 11132243 10516958 14638642


    Sources:
    TEND

  • UMESPIRONE   HTR1A

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • MILNACIPRAN   HTR1A

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18484082


    Sources:
    PharmGKB

  • SERTRALINE   HTR1A

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23733030 21688171 19800133 19590397 18484082 18387740 18047755


    Sources:
    PharmGKB

  • PIROMELATINE   HTR1A

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • VORTIOXETINE HYDROBROMIDE   HTR1A

    Interaction Score: 0.37

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PAROXETINE   HTR1A

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23733030 21688171 19800133 19590397 18484082 18387740 18047755


    Sources:
    PharmGKB

  • ARIPIPRAZOLE LAUROXIL   HTR1A

    Interaction Score: 0.37

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor partial agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TERTATOLOL   HTR1A

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ELTOPRAZINE   HTR1A

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • BUSPIRONE HYDROCHLORIDE   HTR1A

    Interaction Score: 0.37

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor partial agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • QUETIAPINE   HTR1A

    Interaction Score: 0.33

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

    Interaction Info:

    PMIDs:
    17563257 11132243 16918396 17848919 12445705 22120873


    Sources:
    TEND PharmGKB

  • PARDOPRUNOX   HTR1A

    Interaction Score: 0.32

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist
    Direct Interaction yes
    Trial Name pardoprunox, SLV 308

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • GSK163090   HTR1A

    Interaction Score: 0.28

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SARIZOTAN HYDROCHLORIDE   HTR1A

    Interaction Score: 0.28

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AMISULPRIDE   HTR1A

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22120873


    Sources:
    PharmGKB

  • URAPIDIL   HTR1A

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ASENAPINE   HTR1A

    Interaction Score: 0.18

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

    Interaction Info:
    Novel drug target Established target
    Trial Name Asenapine

    PMIDs:
    18308814 10592235


    Sources:
    TdgClinicalTrial

  • CLOZAPINE   HTR1A

    Interaction Score: 0.17

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

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    25560469 12589516 12923612 15261283 15213359 12564641


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • OXYMETAZOLINE HYDROCHLORIDE   HTR1A

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SUMATRIPTAN   HTR1A

    Interaction Score: 0.16

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name MT 400,Treximet
    Novel drug target Established target
    Trial Name NP101,Zelrix

    PMIDs:
    11513839


    Sources:
    TdgClinicalTrial

  • ILOPERIDONE   HTR1A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name iloperidone,Fanapt, Fiapta, Zomaril

    PMIDs:
    23272794


    Sources:
    TdgClinicalTrial

  • FLUOXETINE   HTR1A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19590397 16302021


    Sources:
    PharmGKB

  • ERGOLOID MESYLATES   HTR1A

    Interaction Score: 0.09

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • METHAMPHETAMINE   HTR1A

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19747927


    Sources:
    PharmGKB

  • OLANZAPINE   HTR1A

    Interaction Score: 0.08

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

    Interaction Info:
    Trial Name ALKS 3831
    Trial Name OREX-003, olanzapine plus zonisamide SR
    Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

    PMIDs:
    22120873 17848919 25032030


    Sources:
    TdgClinicalTrial PharmGKB

  • RISPERIDONE   HTR1A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    11132243 22120873


    Sources:
    PharmGKB

  • MIRTAZAPINE   HTR1A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TEND

  • Ensembl: ENSG00000178394

    • Version: 101_38

    Alternate Names:
    HTR1A Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • HopkinsGroom: P08908

    • Version: 11-September-2012

    Alternate Names:
    P08908 Uniprot Accession
    5-HYDROXYTRYPTAMINE RECEPTOR 1A Uniprot Protein Name
    3350 Entrez Gene Id

    Gene Info:
    Interpro Name GPCR, rhodopsin-like, 7TM
    Uniprot Status Swiss-Prot
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

    Publications:

  • TEND: P08908

    • Version: 01-August-2011

    Alternate Names:
    ENSG00000178394 Ensembl Gene Id
    P08908 Uniprot Accession
    5HT1A_HUMAN Uniprot Id

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

    Publications:

  • RussLampel: ENSG00000178394

    • Version: 26-July-2011

    Alternate Names:
    5-HYDROXYTRYPTAMINE 1A RECEPTOR (5-HT-1A) (SEROTONIN RECEPTOR 1A) (5- HT1A) (G-21). [SOURCE:UNIPROT/SWISSPROT;ACC:P08908] Description
    ENSG00000178394 Ensembl Gene Id
    HTR1A Display Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: P08908

    • Version: January-2014

    Alternate Names:
    HTR1A Gene Symbol

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

    Publications:

  • PharmGKB: HTR1A

    • Version: 18-August-2020

    Alternate Names:
    PA192 PharmGKB ID

    Gene Info:

    Publications:
    Kato M et al., 2009, Effect of 5-HT1A gene polymorphisms on antidepressant response in major depressive disorder., Am J Med Genet B Neuropsychiatr Genet
    Illi A et al., 2009, 5-HTR1A, 5-HTR2A, 5-HTR6, TPH1 and TPH2 polymorphisms and major depression., Neuroreport
    Drago A et al., 2008, 5-HT1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies., Int J Neuropsychopharmacol

  • HingoraniCasas: ENSG00000178394

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000178394 Gene Symbol
    HTR1A Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • ChemblInteractions: ADRB2RL1

    • Version: chembl_23

    Alternate Names:
    ADRBRL1 GENE_SYMBOL
    HTR1A GENE_SYMBOL
    5-hydroxytryptamine receptor 1A UNIPROT

    Gene Info:

    Publications:

  • GO: HTR1A

    • Version: 01-February-2022

    Alternate Names:
    ADRB2RL1 GO Gene Synonym
    ADRBRL1 GO Gene Synonym

    Gene Info:

    Gene Categories:
    CELL SURFACE

    Publications:

  • dGene: HTR1A

    • Version: 27-Jun-2013

    Alternate Names:
    3350 Gene ID
    5-HT-1A dGene Synonym
    5-HT1A dGene Synonym

    Gene Info:

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    Publications:

  • TTD: 5-HT 1A receptor

    • Version: 2020.06.01

    Alternate Names:
    HTR1A TTD Gene Abbreviation
    T78709 TTD Target ID

    Gene Info:

    Publications:

  • DTC: HTR1A

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    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