DGIdb - HTR1A Gene Record

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]
1
5-HT<sub>1A</sub> receptor
5-HT 1A receptor
T78709
NM_000524
NP_000515

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
GuideToPharmacology Gene Category Name	5-Hydroxytryptamine receptors
GuideToPharmacology Gene Category ID	1

(9 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.
Johnson et al., 2001, Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain., Eur. 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
Millan et al., 2000, Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states., Synapse
Kaumann, 1983, Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors., Naunyn Schmiedebergs Arch. Pharmacol.
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.
AGHAJANIAN et al., PERSISTENCE OF LYSERGIC ACID DIETHYLAMIDE IN THE PLASMA OF HUMAN SUBJECTS., Clin. Pharmacol. Ther.
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
Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem
LeWitt PA, 2004, Subcutaneously administered apomorphine: pharmacokinetics and metabolism., Neurology
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
Sharif et al., 2009, Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes., Exp. Eye Res.
Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy
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.)
Miyazawa et al., 1991, [Effect of lisuride on experimental cerebral infarction in rats]., Nippon Yakurigaku Zasshi
Newman-Tancredi et al., 1998, Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study., Eur. J. Pharmacol.
Cosi et al., 2001, Agonist, antagonist, and inverse agonist properties of antipsychotics at human recombinant 5-HT(1A) receptors expressed in HeLa cells., Eur. J. Pharmacol.
Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
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
Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
Fornal et al., 1999, Pindolol suppresses serotonergic neuronal activity and does not block the inhibition of serotonergic neurons produced by 8-hydroxy-2-(di-n-propylamino)tetralin in awake cats., J. Pharmacol. Exp. Ther.
Haddjeri et al., 1999, Modulation of the firing activity of rat serotonin and noradrenaline neurons by (+/-)pindolol., Biol. Psychiatry
Smeraldi et al., 1999, Sustained antidepressant effect of sleep deprivation combined with pindolol in bipolar depression. A placebo-controlled trial., Neuropsychopharmacology
Gobert et al., 1999, Modulation of dialysate levels of dopamine, noradrenaline, and serotonin (5-HT) in the frontal cortex of freely-moving rats by (-)-pindolol alone and in association with 5-HT reuptake inhibitors: comparative roles of beta-adrenergic, 5-HT1A, and 5-HT1B receptors., Neuropsychopharmacology
Andrée et al., 1999, Pindolol binding to 5-HT1A receptors in the human brain confirmed with positron emission tomography., Psychopharmacology (Berl.)
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: 3.04

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: 2.43

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor antagonist

Direct Interaction yes

Direct Interaction? False

PMIDs:
9886765 12726821

Sources:
ChemblInteractions GuideToPharmacology
OSEMOZOTAN HTR1A

Interaction Score: 1.82

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
PIZOTYLINE HTR1A

Interaction Score: 1.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
2045831

Sources:
GuideToPharmacology
REPINOTAN HTR1A

Interaction Score: 1.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
10592235

Sources:
GuideToPharmacology
GEPIRONE HTR1A

Interaction Score: 1.22

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: 1.22

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name xaliproden, SR 57746A

PMIDs:
None found

Sources:
TdgClinicalTrial TTD
ZALOSPIRONE HTR1A

Interaction Score: 1.22

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology TTD
BUSPIRONE HTR1A

Interaction Score: 0.95

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Partial agonist

PMIDs:
10064829 10215901 10428422 14769835 11752352 10221756 10027850

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
SARIZOTAN HTR1A

Interaction Score: 0.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15707540 15298067

Sources:
TTD
PINDOLOL HTR1A

Interaction Score: 0.71

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
10490909 10331108 10088139 11752352 10432475 10435400

Sources:
GuideToPharmacology
FLUPAROXAN HTR1A

Interaction Score: 0.61

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
FLESINOXAN HTR1A

Interaction Score: 0.61

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PICLOZOTAN HTR1A

Interaction Score: 0.61

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: 0.61

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BMY-14802 HTR1A

Interaction Score: 0.61

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
XYLOMETAZOLINE HYDROCHLORIDE HTR1A

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TANDOSPIRONE HTR1A

Interaction Score: 0.61

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
LECOZOTAN HYDROCHLORIDE HTR1A

Interaction Score: 0.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ZOLMITRIPTAN HTR1A

Interaction Score: 0.51

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name zolmitriptan,Zomig

Novel drug target Established target

Specific Action of the Ligand Full agonist

PMIDs:
11513839 29352859 9399012

Sources:
TdgClinicalTrial GuideToPharmacology
BIFEPRUNOX HTR1A

Interaction Score: 0.51

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
NARATRIPTAN HTR1A

Interaction Score: 0.49

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Trial Name naratriptan,Naramig, Amerge

PMIDs:
11152011 14728705

Sources:
TdgClinicalTrial GuideToPharmacology
BREXPIPRAZOLE HTR1A

Interaction Score: 0.49

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
VILAZODONE HTR1A

Interaction Score: 0.43

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
15507223 12183683

Sources:
TdgClinicalTrial GuideToPharmacology TTD
LURASIDONE HTR1A

Interaction Score: 0.41

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name lurasidone, SM-13496,Latuda

Novel drug target Established target

PMIDs:
23545936 31636356

Sources:
TdgClinicalTrial PharmGKB
FLIBANSERIN HTR1A

Interaction Score: 0.41

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
26412054 12177684 12890707

Sources:
TdgClinicalTrial GuideToPharmacology TTD
ARIPIPRAZOLE HTR1A

Interaction Score: 0.38

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 GuideToPharmacology
FLUVOXAMINE HTR1A

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23733030 21688171 19800133 19590397 18484082 18387740 18047755

Sources:
PharmGKB
LISURIDE HTR1A

Interaction Score: 0.34

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Trial Name -

PMIDs:
1678728 2887435 11224054 12373423 18691132 1783326

Sources:
TdgClinicalTrial TEND GuideToPharmacology
VILAZODONE HYDROCHLORIDE HTR1A

Interaction Score: 0.3

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
ROTIGOTINE HTR1A

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
18704368 18691132

Sources:
TEND
IPSAPIRONE HTR1A

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
UMESPIRONE HTR1A

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
TRAZODONE HTR1A

Interaction Score: 0.3

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
ZIPRASIDONE HTR1A

Interaction Score: 0.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
11513838 11910268 14728084 12923612 10924666 11132243 10516958 14638642

Sources:
TEND GuideToPharmacology
VORTIOXETINE HTR1A

Interaction Score: 0.27

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name Lu AA21004

Novel drug target Established target

Specific Action of the Ligand Partial agonist

PMIDs:
21486038 16290165

Sources:
TdgClinicalTrial GuideToPharmacology
METHYSERGIDE HTR1A

Interaction Score: 0.25

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
1838579 14501155 11049861 14581123 14517765

Sources:
TdgClinicalTrial TEND
5-MEO-DMT HTR1A

Interaction Score: 0.24

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
26477571

Sources:
DTC
MILNACIPRAN HTR1A

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18484082

Sources:
PharmGKB
LYSERGIDE HTR1A

Interaction Score: 0.24

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
14209776

Sources:
GuideToPharmacology
SERTRALINE HTR1A

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23733030 21688171 19800133 19590397 18484082 18387740 18047755

Sources:
PharmGKB
PIROMELATINE HTR1A

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
NAFADOTRIDE HTR1A

Interaction Score: 0.2

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
TIOSPIRONE HTR1A

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
VORTIOXETINE HYDROBROMIDE HTR1A

Interaction Score: 0.2

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FROVATRIPTAN HTR1A

Interaction Score: 0.2

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
ARIPIPRAZOLE LAUROXIL HTR1A

Interaction Score: 0.2

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
WAY-100,635 HTR1A

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
ELTOPRAZINE HTR1A

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ELETRIPTAN HTR1A

Interaction Score: 0.2

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
11513839

Sources:
GuideToPharmacology
BUSPIRONE HYDROCHLORIDE HTR1A

Interaction Score: 0.2

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
PAROXETINE HTR1A

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23733030 21688171 19800133 19590397 18484082 18387740 18047755

Sources:
PharmGKB
QUETIAPINE HTR1A

Interaction Score: 0.18

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
17563257 11132243 16918396 17848919 12445705 22120873

Sources:
TEND GuideToPharmacology PharmGKB
PARDOPRUNOX HTR1A

Interaction Score: 0.17

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
CABERGOLINE HTR1A

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
18992242 18691132 10641988

Sources:
GuideToPharmacology
GSK163090 HTR1A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CYAMEMAZINE HTR1A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SARIZOTAN HYDROCHLORIDE HTR1A

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TERTATOLOL HTR1A

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHEMBL38288 HTR1A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
AMISULPRIDE HTR1A

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22120873

Sources:
PharmGKB
YOHIMBINE HTR1A

Interaction Score: 0.13

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
10611634 6136920

Sources:
GuideToPharmacology
PERGOLIDE HTR1A

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
18691132 10641988

Sources:
GuideToPharmacology
ILOPERIDONE HTR1A

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name iloperidone,Fanapt, Fiapta, Zomaril

Specific Action of the Ligand Antagonist

PMIDs:
23272794

Sources:
TdgClinicalTrial GuideToPharmacology
URAPIDIL HTR1A

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
RACLOPRIDE HTR1A

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
RIZATRIPTAN HTR1A

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BMY-7378 HTR1A

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PIPAMPERONE HTR1A

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
ASENAPINE HTR1A

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Asenapine

Endogenous Drug? False

PMIDs:
18308814 10592235

Sources:
TdgClinicalTrial GuideToPharmacology
SUMATRIPTAN HTR1A

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Trial Name MT 400,Treximet

PMIDs:
11513839

Sources:
TdgClinicalTrial GuideToPharmacology
OCAPERIDONE HTR1A

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
OXYMETAZOLINE HYDROCHLORIDE HTR1A

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CLOZAPINE HTR1A

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Full agonist

PMIDs:
25560469 12589516 12923612 15261283 15213359 12564641

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB
APOMORPHINE HTR1A

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
18691132 15037665

Sources:
GuideToPharmacology
MESORIDAZINE HTR1A

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
DONITRIPTAN HTR1A

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BRL-15,572 HTR1A

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CAPESEROD HTR1A

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BROMOCRIPTINE HTR1A

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
18691132 10641988

Sources:
GuideToPharmacology
FLUOXETINE HTR1A

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19590397 16302021

Sources:
PharmGKB
QUINPIROLE HTR1A

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SPIROXATRINE HTR1A

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CHLORPROMAZINE HTR1A

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
9760039 11755134

Sources:
GuideToPharmacology
8-OH-DPAT HTR1A

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
OLANZAPINE HTR1A

Interaction Score: 0.05

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 GuideToPharmacology PharmGKB
PIRIBEDIL HTR1A

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ERGOLOID MESYLATES HTR1A

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
TERGURIDE HTR1A

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
METHAMPHETAMINE HTR1A

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19747927

Sources:
PharmGKB
ROXINDOLE HTR1A

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
XANOMELINE HTR1A

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
ZOTEPINE HTR1A

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
RISPERIDONE HTR1A

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
11132243 22120873

Sources:
GuideToPharmacology PharmGKB
SPIPERONE HTR1A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
MIRTAZAPINE HTR1A

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
SERTINDOLE HTR1A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SEROTONIN HTR1A

Interaction Score: 0.03

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? True

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
KETANSERIN HTR1A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
THIORIDAZINE HTR1A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
RITANSERIN HTR1A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
METITEPINE HTR1A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
FLUSPIRILENE HTR1A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PIMOZIDE HTR1A

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
HALOPERIDOL HTR1A

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
12629531

Sources:
GuideToPharmacology

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:
GuideToPharmacology: 3350
- Version: 29-September-2020
Alternate Names:

5286 HUGO Gene ID

5286 HUGO Gene Symbol

5-hydroxytryptamine receptor 1A HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name 5-Hydroxytryptamine receptors

GuideToPharmacology Gene Category ID 1

Gene Categories:

G PROTEIN COUPLED RECEPTOR

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:
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:
GO: HTR1A
- Version: 01-May-2021
Alternate Names:

ADRB2RL1 GO Gene Synonym

ADRBRL1 GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE

Publications:
DTC: HTR1A
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

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

Mechanism of Interaction	Serotonin 1a (5-HT1a) receptor antagonist
Direct Interaction	yes
Direct Interaction?	False

Endogenous Drug?	False
Specific Action of the Ligand	Antagonist

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False

Specific Action of the Ligand	Partial agonist
Endogenous Drug?	False

Trial Name	zolmitriptan,Zomig
Novel drug target	Established target
Specific Action of the Ligand	Full agonist

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

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

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

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

Trial Name	Lu AA21004
Novel drug target	Established target
Specific Action of the Ligand	Partial agonist

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

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

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

ENSG00000178394	Ensembl Gene Id
P08908	Uniprot Accession
5HT1A_HUMAN	Uniprot Id

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

5286	HUGO Gene ID
5286	HUGO Gene Symbol
5-hydroxytryptamine receptor 1A	HUGO Gene Name

ADRBRL1	GENE_SYMBOL
HTR1A	GENE_SYMBOL
5-hydroxytryptamine receptor 1A	UNIPROT

HTR1A Gene Record

HTR1A 3350 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

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

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 9886765 12726821

Sources: ChemblInteractions GuideToPharmacology

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

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 2045831

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 10592235

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: Trial Name Gepirone Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: GuideToPharmacology TTD

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

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

PMIDs: 10064829 10215901 10428422 14769835 11752352 10221756 10027850

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15707540 15298067

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 10490909 10331108 10088139 11752352 10432475 10435400

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor antagonist

Direct Interaction yes

Direct Interaction? False

PMIDs:
9886765 12726821

Sources:
ChemblInteractions GuideToPharmacology

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
2045831

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
10592235

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Gepirone

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name xaliproden, SR 57746A

PMIDs:
None found

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology TTD

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Partial agonist

PMIDs:
10064829 10215901 10428422 14769835 11752352 10221756 10027850

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
15707540 15298067

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
10490909 10331108 10088139 11752352 10432475 10435400

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name zolmitriptan,Zomig

Novel drug target Established target

Specific Action of the Ligand Full agonist

PMIDs:
11513839 29352859 9399012

Sources:
TdgClinicalTrial GuideToPharmacology

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