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]
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:

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

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

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

Trial Name	zolmitriptan,Zomig
Novel drug target	Established target

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

Trial Name	naratriptan,Naramig, Amerge
Novel drug target	Established target

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

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

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

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

PMIDs: 9886765 12726821

Sources: ChemblInteractions

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: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 1678728 2887435 11224054 12373423 18691132 1783326

Sources: TdgClinicalTrial TEND

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

PMIDs: 15507223 12183683

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15707540 15298067

Sources: TTD

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

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 26477571

Sources: DTC

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: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

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:

PMIDs: None found

Sources: TTD

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

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 11513839 29352859 9399012

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 23545936 31636356

Sources: TdgClinicalTrial PharmGKB

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

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

PMIDs:
9886765 12726821

Sources:
ChemblInteractions

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:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
1678728 2887435 11224054 12373423 18691132 1783326

Sources:
TdgClinicalTrial TEND

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:

Trial Name vilazodone hydrochloride, SB 659746A

Novel drug target Established target

PMIDs:
15507223 12183683

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

n/a

PMIDs:
15707540 15298067

Sources:
TTD

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

Interaction Types & Directionality:

agonist (activating)

PMIDs:
26477571

Sources:
DTC

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:

n/a

PMIDs:
None found

Sources:
DTC

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)

PMIDs:
None found

Sources:
TTD

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

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name zolmitriptan,Zomig

Novel drug target Established target

PMIDs:
11513839 29352859 9399012

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name lurasidone, SM-13496,Latuda

Novel drug target Established target

PMIDs:
23545936 31636356

Sources:
TdgClinicalTrial PharmGKB

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

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name naratriptan,Naramig, Amerge

Novel drug target Established target

PMIDs:
11152011 14728705

Sources:
TdgClinicalTrial

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