DGIdb - HTR2A Gene Record

HTR2A 3356 Druggable GenomeDrug Resistance

Alternate Names:

3356
5-HYDROXYTRYPTAMINE RECEPTOR 2A
HTR2A
5-HT2A
HTR2
182135
5293
ENSG00000102468
OTTHUMG00000016881
Serotonin receptor 2A
5-HT-2
5-HT-2A
P28223
5HT2A_HUMAN
PA193
6
5-HT<sub>2A</sub> receptor
5-HYDROXYTRYPTAMINE 2A RECEPTOR (5-HT-2A) (SEROTONIN RECEPTOR 2A) (5- HT-2). [SOURCE:UNIPROT/SWISSPROT;ACC:P28223]
5-HT 2A receptor
T32060
NP_000612
NM_000621

Gene Info:

Target Main Class	Receptors
Target Subclass	Rhodopsin
Transmembrane Helix Count	7
Target Subclass	GPCR
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Interpro Acc	IPR000276
Uniprot Status	Swiss-Prot
Uniprot Evidence	1: Evidence at protein level
Interpro Name	GPCR, rhodopsin-like, 7TM
Interpro Type	Family
Human Readable Name	DRUGGABLE GENOME
Interpro Short Name	7TM_GPCR_Rhodpsn
Target Class	Receptors
Gene Biotype	PROTEIN_CODING
GuideToPharmacology Gene Category Name	5-Hydroxytryptamine receptors
GuideToPharmacology Gene Category ID	1

(10 More Sources)

Gene Categories: Category Details

KINASE
DRUG RESISTANCE
G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Roth et al., 1994, Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors., J. Pharmacol. Exp. Ther.
Kusumi et al., 2000, Differential effects of subchronic treatments with atypical antipsychotic drugs on dopamine D2 and serotonin 5-HT2A receptors in the rat brain., J Neural Transm (Vienna)
Yamada et al., 1995, Serotonin2 (5-HT2) receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) inhibits chlorpromazine- and haloperidol-induced hypothermia in mice., Biol. Pharm. Bull.
Maeda et al., 2014, Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator., J. Pharmacol. Exp. Ther.
Kongsamut et al., 1996, Iloperidone binding to human and rat dopamine and 5-HT receptors., Eur. J. Pharmacol.
Hesselink, 2002, Iloperidone (Novartis)., IDrugs
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Serretti et al., Serotonin receptor 2A, 2C, 1A genes and response to lithium prophylaxis in mood disorders., J Psychiatr Res
Sharif, 2010, Serotonin-2 receptor agonists as novel ocular hypotensive agents and their cellular and molecular mechanisms of action., Curr Drug Targets
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.
Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem
Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy
Kumar B et al., 2018, Lumateperone: a new treatment approach for neuropsychiatric disorders., Drugs Today (Barc)
Antkiewicz-Michaluk, The influence of chronic treatment with antidepressant neuroleptics on the central serotonin system., Pol J Pharmacol Pharm
Wander et al., 1987, Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro., Eur. J. Pharmacol.
Nash et al., 1994, Effect of the R(-) and S(+) isomers of MDA and MDMA on phosphatidyl inositol turnover in cultured cells expressing 5-HT2A or 5-HT2C receptors., Neurosci. Lett.
Lyon et al., 1986, 3,4-Methylenedioxymethamphetamine (MDMA): stereoselective interactions at brain 5-HT1 and 5-HT2 receptors., Psychopharmacology (Berl.)
Leysen et al., 1994, Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity., J Clin Psychiatry
Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
Nakamura et al., 2001, Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism., Eur. J. Pharmacol.
Kobayashi et al., 1996, Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems., Eur. J. Pharmacol.
Honda et al., 2003, Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors., Eur. J. Pharmacol.
Mestres J et al., 2011, Linking pharmacology to clinical reports: cyclobenzaprine and its possible association with serotonin syndrome., Clin Pharmacol Ther
Grinshpoon et al., 2000, Beneficial effect of the addition of the 5-HT 2A/2C and alpha2 antagonist mianserin to ongoing haloperidol treatment in drug-resistant chronically hospitalized schizophrenic patients., Eur. Psychiatry
Deeks, 2015, Flibanserin: First Global Approval., Drugs
Borsini et al., 2002, Pharmacology of flibanserin., CNS Drug Rev
Invernizzi et al., 2003, Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors., Br. J. Pharmacol.
Peroutka et al., 1981, Two distinct central serotonin receptors with different physiological functions., Science
Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
Citrome, 2011, Role of sublingual asenapine in treatment of schizophrenia., Neuropsychiatr Dis Treat
McIntyre et al., 2007, A preclinical and clinical rationale for quetiapine in mood syndromes., Expert Opin Pharmacother
Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.
Goldstein, 1999, Quetiapine fumarate (Seroquel): a new atypical antipsychotic., Drugs Today
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
Yatham et al., 2005, Atypical antipsychotics in bipolar depression: potential mechanisms of action., J Clin Psychiatry
Choi et al., 2004, Synthesis, receptor binding and functional studies of mesoridazine stereoisomers., Bioorg. Med. Chem. Lett.
Rauser et al., 2001, Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor., J. Pharmacol. Exp. Ther.
Herrick-Davis et al., 2000, Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors., J. Pharmacol. Exp. Ther.
Hietala et al., 2001, Sertindole is a serotonin 5-HT2c inverse agonist and decreases agonist but not antagonist binding to 5-HT2c receptors after chronic treatment., Psychopharmacology (Berl.)
Schreiber et al., 1994, Blockade of the discriminative stimulus effects of DOI by MDL 100,907 and the 'atypical' antipsychotics, clozapine and risperidone., Eur. J. Pharmacol.
Lindström et al., 2006, Sertindole: efficacy and safety in schizophrenia., Expert Opin Pharmacother
Kasho et al., 1998, Serotonin enhances the production of type IV collagen by human mesangial cells., Kidney Int.
Egan et al., 1998, Agonist activity of LSD and lisuride at cloned 5HT2A and 5HT2C receptors., Psychopharmacology (Berl.)
Bixo et al., 2001, Binding of [3H]paroxetine to serotonin uptake sites and of [3H]lysergic acid diethylamide to 5-HT2A receptors in platelets from women with premenstrual dysphoric disorder during gonadotropin releasing hormone treatment., Psychoneuroendocrinology
Meyer et al., 2001, The effect of paroxetine on 5-HT(2A) receptors in depression: an [(18)F]setoperone PET imaging study., Am J Psychiatry
Kato M et al., 2009, 5-HT2A gene variants influence specific and different aspects of antidepressant response in Japanese and Italian mood disorder patients., Psychiatry Res
Wilkie MJ et al., 2009, Polymorphisms in the SLC6A4 and HTR2A genes influence treatment outcome following antidepressant therapy., Pharmacogenomics J
Tanaka M et al., 2008, Genetic polymorphisms in the 5-hydroxytryptamine type 3B receptor gene and paroxetine-induced nausea., Int J Neuropsychopharmacol
Murphy GM Jr et al., 2003, Pharmacogenetics of antidepressant medication intolerance., Am J Psychiatry
Foster RH et al., 1997, Paroxetine : a review of its pharmacology and therapeutic potential in the management of panic disorder., CNS Drugs
Newcombe F et al., 1969, Alkaloids of the leaves of Voacanga schweinfurthii Stapf., Planta Med
Canton et al., 1994, Competitive antagonism of serotonin (5-HT)2C and 5-HT2A receptor-mediated phosphoinositide (PI) turnover by clozapine in the rat: a comparison to other antipsychotics., Neurosci. Lett.
Costall et al., 1995, Behavioural interactions between 5-hydroxytryptophan, neuroleptic agents and 5-HT receptor antagonists in modifying rodent responding to aversive situations., Br. J. Pharmacol.
Morisset et al., 1999, Atypical neuroleptics enhance histamine turnover in brain via 5-Hydroxytryptamine2A receptor blockade., J. Pharmacol. Exp. Ther.
Andree et al., 1986, Differential effect of subchronic treatment with various neuroleptic agents on serotonin2 receptors in rat cerebral cortex., J. Neurochem.
Burki, 1986, Binding of psychoactive drugs to rat brain amine receptors, measured ex vivo, and their effects on the metabolism of biogenic amines., Naunyn Schmiedebergs Arch. Pharmacol.
Reist et al., 2004, Inter-relationships of intermediate phenotypes for serotonin function, impulsivity, and a 5-HT2A candidate allele: His452Tyr., Mol. Psychiatry
McDonald et al., 2003, Enhancement of latent inhibition by two 5-HT2A receptor antagonists only when given at both pre-exposure and conditioning., Psychopharmacology (Berl.)
Heiser et al., 2004, Effects of clozapine and its metabolites on the 5-HT2 receptor system in cortical and hippocampal cells in vitro., Prog. Neuropsychopharmacol. Biol. Psychiatry
Broderick et al., 2004, Clozapine and cocaine effects on dopamine and serotonin release in nucleus accumbens during psychostimulant behavior and withdrawal., Prog. Neuropsychopharmacol. Biol. Psychiatry
Travis et al., 1998, 5-HT2A receptor blockade in patients with schizophrenia treated with risperidone or clozapine. A SPET study using the novel 5-HT2A ligand 123I-5-I-R-91150., Br J Psychiatry
Arranz et al., 1996, Analysis of a structural polymorphism in the 5-HT2A receptor and clinical response to clozapine., Neurosci. Lett.
Salloum NC et al., 2014, Towards the clinical implementation of pharmacogenetics in bipolar disorder., BMC Med
Muntasir HA et al., 2006, Inverse agonist activity of sarpogrelate, a selective 5-HT2A-receptor antagonist, at the constitutively active human 5-HT2A receptor., J Pharmacol Sci
Friedman, 2013, Pimavanserin for the treatment of Parkinson's disease psychosis., Expert Opin Pharmacother
Stark et al., 2007, Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT 2A receptors: functional receptor-binding and in vivo electrophysiological studies., Psychopharmacology (Berl.)
Bortolozzi et al., 2007, In vivo actions of aripiprazole on serotonergic and dopaminergic systems in rodent brain., Psychopharmacology (Berl.)
Meltzer et al., 2003, Serotonin receptors: their key role in drugs to treat schizophrenia., Prog. Neuropsychopharmacol. Biol. Psychiatry
de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
Anttila et al., 2001, A review of the pharmacological and clinical profile of mirtazapine., CNS Drug Rev
Westenberg, 1999, Pharmacology of antidepressants: selectivity or multiplicity?, J Clin Psychiatry
Gorman, 1999, Mirtazapine: clinical overview., J Clin Psychiatry
Laakmann et al., 1999, Effects of mirtazapine on growth hormone, prolactin, and cortisol secretion in healthy male subjects., Psychoneuroendocrinology
Waldinger et al., 2000, Treatment of hot flushes with mirtazapine: four case reports., Maturitas
Nutt, 1999, Care of depressed patients with anxiety symptoms., J Clin Psychiatry
Celada P et al., 2004, The therapeutic role of 5-HT1A and 5-HT2A receptors in depression., J Psychiatry Neurosci
Pawlyk AC et al., 2006, Effects of the 5-HT2A antagonist mirtazapine in rat models of thermoregulation., Brain Res
Deeks ED et al., 2010, Blonanserin: a review of its use in the management of schizophrenia., CNS Drugs
Bisson WH et al., 2007, Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs., Proc Natl Acad Sci U S A
Cohen, Risperidone., Pharmacotherapy
Megens et al., 1994, Survey on the pharmacodynamics of the new antipsychotic risperidone., Psychopharmacology (Berl.)
He et al., 1995, A pharmacological, pharmacokinetic and clinical overview of risperidone, a new antipsychotic that blocks serotonin 5-HT2 and dopamine D2 receptors., Int Clin Psychopharmacol
Yamada et al., 2002, Prediction and assessment of extrapyramidal side effects induced by risperidone based on dopamine D(2) receptor occupancy., Synapse
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
Eckler et al., 2003, Nefazodone in the rat: mimicry and antagonism of [-]-DOM-induced stimulus control., Pharmacol. Biochem. Behav.
Hidalgo et al., 1999, Nefazodone in post-traumatic stress disorder: results from six open-label trials., Int Clin Psychopharmacol
Davis et al., 1997, Nefazodone. A review of its pharmacology and clinical efficacy in the management of major depression., Drugs
Avila et al., 2003, Does nefazodone improve both depression and Parkinson disease? A pilot randomized trial., J Clin Psychopharmacol
Horton et al., 1999, Akinetopsia from nefazodone toxicity., Am. J. Ophthalmol.
Taylor et al., 1995, Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug., J Clin Psychiatry
Meyer et al., 1999, The effects of single dose nefazodone and paroxetine upon 5-HT2A binding potential in humans using [18F]-setoperone PET., Psychopharmacology (Berl.)
Keks et al., 1999, Risperidone (Risperdal): clinical experience with a new antipsychosis drug., Expert Opin Investig Drugs
Uchida et al., 2007, Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine., Life Sci.
Fenton et al., 2005, Risperidone: a review of its use in the treatment of bipolar mania., CNS Drugs
Maffioletti E et al., 2020, Association study between HTR2A rs6313 polymorphism and early response to risperidone and olanzapine in schizophrenia patients., Drug Dev Res
López-Rodríguez R et al., 2013, Pharmacodynamic genetic variants related to antipsychotic adverse reactions in healthy volunteers., Pharmacogenomics
Correia CT et al., 2010, Pharmacogenetics of risperidone therapy in autism: association analysis of eight candidate genes with drug efficacy and adverse drug reactions., Pharmacogenomics J
Angelucci F et al., 2009, Delusion symptoms and response to antipsychotic treatment are associated with the 5-HT2A receptor polymorphism (102T/C) in Alzheimer's disease: a 3-year follow-up longitudinal study., J Alzheimers Dis
Corena-McLeod M, 2015, Comparative Pharmacology of Risperidone and Paliperidone., Drugs R D
Laika B et al., 2010, Pharmacogenetics and olanzapine treatment: CYP1A2*1F and serotonergic polymorphisms influence therapeutic outcome., Pharmacogenomics J
Ujike H et al., 2008, Multiple genetic factors in olanzapine-induced weight gain in schizophrenia patients: a cohort study., J Clin Psychiatry
Thomas P et al., 2008, Correlates of response to Olanzapine in a North Indian Schizophrenia sample., Psychiatry Res
Moresco et al., 2004, Cerebral D2 and 5-HT2 receptor occupancy in Schizophrenic patients treated with olanzapine or clozapine., J. Psychopharmacol. (Oxford)
Bymaster et al., 1999, Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro., Schizophr. Res.
Padín et al., 2006, Parallel regulation by olanzapine of the patterns of expression of 5-HT2A and D3 receptors in rat central nervous system and blood cells., Neuropharmacology
Sharpley et al., 2005, Olanzapine increases slow wave sleep and sleep continuity in SSRI-resistant depressed patients., J Clin Psychiatry
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
Aly SA et al., 2009, Assessment of binding affinity to 5-hydroxytryptamine 2A (5-HT2A) receptor and inverse agonist activity of naftidrofuryl: comparison with those of sarpogrelate., J Pharmacol Sci
Govitrapong et al., 2002, Platelet serotonin transporter in schizophrenic patients with and without neuroleptic treatment., Neurochem. Int.
Govitrapong et al., 2000, Platelet 5-HT(2A) receptors in schizophrenic patients with and without neuroleptic treatment., Psychiatry Res
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Kim DH et al., 2009, Building a better antipsychotic: receptor targets for the treatment of multiple symptom dimensions of schizophrenia., Neurotherapeutics
Nguyen et al., 1989, Down-regulation of tryptamine binding sites following chronic molindone administration. A comparison with responses of dopamine and 5-hydroxytryptamine receptors., Naunyn Schmiedebergs Arch. Pharmacol.
Castilho et al., 1999, Antinociception elicited by aversive stimulation of the inferior colliculus., Pharmacol. Biochem. Behav.
Shaw et al., 2000, Role of the 5-HT(2A)receptor and alpha(1)-adrenoceptor in the contractile response of rat pulmonary artery to 5-HT in the presence and absence of nitric oxide., Pulm Pharmacol Ther
Connor et al., 2001, Second messengers in platelet aggregation evoked by serotonin and A23187, a calcium ionophore., Life Sci.
Geerts et al., 1999, Involvement of 5-HT1B receptors in collar-induced hypersensitivity to 5-hydroxytryptamine of the rabbit carotid artery., Br. J. Pharmacol.
Prins et al., 2001, Characterization of the receptors involved in the 5-HT-induced excitation of canine antral longitudinal muscle., Br. J. Pharmacol.
Cussac et al., 2008, Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells., Eur. J. Pharmacol.
LeWitt PA, 2004, Subcutaneously administered apomorphine: pharmacokinetics and metabolism., Neurology
Görnemann T et al., 2008, Characterization of the molecular fragment that is responsible for agonism of pergolide at serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A receptors., J Pharmacol Exp Ther
Nabeshima et al., 1989, Effect of minaprine on cycloheximide-induced amnesia in mice., Eur. J. Pharmacol.
Muramatsu et al., 1988, 5-HT2 antagonists and minaprine block the 5-HT-induced inhibition of dopamine release from rat brain striatal slices., Eur. J. Pharmacol.
Kodama et al., 1992, Protective effect of minaprine against the abnormal changes of 2-deoxyglucose uptake by rat hippocampal slices induced by hypoxia/hypoglycemia., Jpn. J. Pharmacol.
Bizière et al., 1985, Minaprine, a new drug with antidepressant properties., Drugs Exp Clin Res
George et al., 2013, Newer antipsychotics and upcoming molecules for schizophrenia., Eur. J. Clin. Pharmacol.
Uher R et al., 2009, Genetic predictors of response to antidepressants in the GENDEP project., Pharmacogenomics J
Sanchez C et al., 2014, A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike?, Int Clin Psychopharmacol
Li et al., 2003, A comparison of the effects of loxapine with ziprasidone and thioridazine on the release of dopamine and acetylcholine in the prefrontal cortex and nucleus accumbens., Psychopharmacology (Berl.)
Panconesi et al., 1994, Comparison between venoconstrictor effects of sumatriptan and ergotamine in migraine patients., Headache
Bom et al., 1989, Reduction of cephalic arteriovenous shunting by ergotamine is not mediated by 5-HT1-like or 5-HT2 receptors., Br. J. Pharmacol.
Schotte et al., 1996, Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding., Psychopharmacology (Berl.)
Adolph O et al., 2012, Promethazine inhibits NMDA-induced currents - new pharmacological aspects of an old drug., Neuropharmacology
Sharma A et al., 2003, Classic histamine H1 receptor antagonists: a critical review of their metabolic and pharmacokinetic fate from a bird's eye view., Curr Drug Metab
POWE CE et al., 1962, Propiomazine hydrochloride in obstetrical analgesia. A controlled study of 520 patients., JAMA
Tiwari AK et al., 2013, Analysis of 34 candidate genes in bupropion and placebo remission., Int J Neuropsychopharmacol
Mansbach et al., Blockade of drug-induced deficits in prepulse inhibition of acoustic startle by ziprasidone., Pharmacol. Biochem. Behav.
Stahl et al., 2003, The psychopharmacology of ziprasidone: receptor-binding properties and real-world psychiatric practice., J Clin Psychiatry
Kast et al., 2007, Treatment schedules for 5-HT2A blocking in progressive multifocal leukoencephalopathy using risperidone or ziprasidone., Bone Marrow Transplant.
Ichikawa et al., 2002, Atypical antipsychotic drugs, quetiapine, iloperidone, and melperone, preferentially increase dopamine and acetylcholine release in rat medial prefrontal cortex: role of 5-HT1A receptor agonism., Brain Res.
Lu et al., 2002, A case of ziprasidone-induced mania and the role of 5-HT2A in mood changes induced by atypical antipsychotics., J Clin Psychiatry
Mamo et al., 2004, A PET study of dopamine D2 and serotonin 5-HT2 receptor occupancy in patients with schizophrenia treated with therapeutic doses of ziprasidone., Am J Psychiatry
Rashid et al., 2002, Effects of sarpogrelate, a novel 5-HT2 antagonist, on 5-HT-induced endothelium-dependent relaxations in porcine coronary artery., Jpn. J. Pharmacol.
Hoenicke et al., 1992, The discriminative stimulus effects of clozapine in pigeons: involvement of 5-hydroxytryptamine1C and 5-hydroxytryptamine2 receptors., J. Pharmacol. Exp. Ther.
Callaway et al., 1992, Serotonin 5-HT1-like receptors mediate hyperactivity in rats induced by 3,4-methylenedioxymethamphetamine., Neuropsychopharmacology
Calka et al., Effect of cyproheptadine on serum leptin levels., Adv Ther
Ivgy-May et al., 2015, Esmirtazapine in non-elderly adult patients with primary insomnia: efficacy and safety from a randomized, 6-week sleep laboratory trial., Sleep Med.
Sánchez Martín A et al., 2013, Impact of pharmacogenetics on CNS side effects related to efavirenz., Pharmacogenomics
Conn et al., 1987, Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors., J. Pharmacol. Exp. Ther.
Marek et al., 1992, A comparison of trazodone and fluoxetine: implications for a serotonergic mechanism of antidepressant action., Psychopharmacology (Berl.)
Pazzagli et al., 1999, Trazodone increases extracellular serotonin levels in the frontal cortex of rats., Eur. J. Pharmacol.
Marcoli et al., 2001, Inhibitory presynaptic 5-hydroxytryptamine(2A) receptors regulate evoked glutamate release from rat cerebellar mossy fibers., J. Pharmacol. Exp. Ther.
Luparini et al., 2004, A cortical GABA-5HT interaction in the mechanism of action of the antidepressant trazodone., Prog. Neuropsychopharmacol. Biol. Psychiatry
Stryjer R et al., 2003, Treatment of neuroleptic-induced akathisia with the 5-HT2A antagonist trazodone., Clin Neuropharmacol
Balsara JJ et al., 2005, Effects of the antidepressant trazodone, a 5-HT 2A/2C receptor antagonist, on dopamine-dependent behaviors in rats., Psychopharmacology (Berl)
Cargnin S et al., 2014, Combined effect of common gene variants on response to drug withdrawal therapy in medication overuse headache., Eur J Clin Pharmacol
Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr
Maj et al., 1977, Doxepin as a blocker of central serotonin receptors., Pharmakopsychiatr Neuropsychopharmakol
Lohoff FW et al., 2013, Serotonin receptor 2A (HTR2A) gene polymorphism predicts treatment response to venlafaxine XR in generalized anxiety disorder., Pharmacogenomics J
Demirbugen Oz M et al., 2018, The relationship between the serotonin 2A receptor gene -1438A/G and 102T/C polymorphisms and citalopram/sertraline-induced nausea in major depressed patients., Hum Psychopharmacol
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PIMAVANSERIN HTR2A

Interaction Score: 1.75

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Pimavanserin

Details of the Assay for Interaction Ki determined in membrane radioligand binding assay.

PMIDs:
24016069

Sources:
TdgClinicalTrial GuideToPharmacology TTD
NELOTANSERIN HTR2A

Interaction Score: 0.87

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor inverse agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
TEMANOGREL HTR2A

Interaction Score: 0.87

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor inverse agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
PRUVANSERIN HTR2A

Interaction Score: 0.87

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
IFERANSERIN HTR2A

Interaction Score: 0.87

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name iferanserin ointment

Novel drug target Established target

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
BLONANSERIN HTR2A

Interaction Score: 0.66

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
20030420

Sources:
GuideToPharmacology TTD
CYCLOBENZAPRINE HTR2A

Interaction Score: 0.52

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8884233 12498911 21975349

Sources:
TdgClinicalTrial TEND TTD
VOLINANSERIN HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Trial Name volinanserin

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology
EPLIVANSERIN HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PIMAVANSERIN TARTRATE HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor inverse agonist

PMIDs:
None found

Sources:
ChemblInteractions
AMESERGIDE HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SERGOLEXOLE HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
MINAPRINE HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2530096 2975224 1361012 3836113

Sources:
TdgClinicalTrial TEND
SARPOGRELATE HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
19672037 17031071

Sources:
GuideToPharmacology TTD
NEFAZODONE HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
7855217 12873632 10220119 9098663 14520130 10577608 7649970 10435395

Sources:
TdgClinicalTrial TEND GuideToPharmacology
PALIPERIDONE HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name paliperidone ER, paliperidone palmitate

Novel drug target Established target

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
7520908 7524043 7531353 7542676 11132243 12211096

Sources:
TdgClinicalTrial ChemblInteractions TEND
NEMIFITIDE HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name INN-00835, nemifitide

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
LUMATEPERONE HTR2A

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name ITI-007, ITI-722

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
30596390

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD
THIOTHIXENE HTR2A

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
10821438 8593484

Sources:
ChemblInteractions GuideToPharmacology
TRAZODONE HTR2A

Interaction Score: 0.34

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name trazodone extended release, DDS-04A,Oleptro

Specific Action of the Ligand Antagonist

PMIDs:
3039120 1365657 10594316 11714900 15610924 7855217 12782915 15614572

Sources:
TdgClinicalTrial TEND GuideToPharmacology
CYPROHEPTADINE HTR2A

Interaction Score: 0.34

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12233819 1403790 1358088 16418149 12498911

Sources:
TdgClinicalTrial TEND
MESORIDAZINE HTR2A

Interaction Score: 0.33

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
15357957 11561066 10991983

Sources:
TdgClinicalTrial TEND GuideToPharmacology
CHLORPROTHIXENE HTR2A

Interaction Score: 0.31

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
3774629 2891550

Sources:
TdgClinicalTrial ChemblInteractions TEND
ESMIRTAZAPINE HTR2A

Interaction Score: 0.29

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Trial Name esmirtazapine, ORG-4420

Novel drug target Established target

PMIDs:
26047892

Sources:
TdgClinicalTrial
FLIBANSERIN HTR2A

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Direct Interaction? True

Endogenous Drug? False

PMIDs:
26412054 12177684 12890707

Sources:
TdgClinicalTrial GuideToPharmacology TTD
TRELANSERIN HTR2A

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

Trial Name trelanserin, SL 65.0472

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
MIRTAZAPINE HTR2A

Interaction Score: 0.28

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

Trial Name mirtazapine,Remeron, Remeron SolTab, Reflex

PMIDs:
11607047 10446734 10446735 10451911 11063897 10446738 15309042 17067560

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
MIDOMAFETAMINE HTR2A

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
7824160 2871581

Sources:
TTD
BREXPIPRAZOLE HTR2A

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

Trial Name OPC-34712

PMIDs:
24947465

Sources:
TdgClinicalTrial ChemblInteractions
PROPIOMAZINE HTR2A

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 19110200 22507664 12678691 14488364

Sources:
TdgClinicalTrial TEND
ROLUPERIDONE HYDROCHLORIDE HTR2A

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
MOLINDONE HYDROCHLORIDE HTR2A

Interaction Score: 0.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ASENAPINE MALEATE HTR2A

Interaction Score: 0.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ABAPERIDONE HTR2A

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
MESORIDAZINE BESYLATE HTR2A

Interaction Score: 0.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LURASIDONE HYDROCHLORIDE HTR2A

Interaction Score: 0.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RISPERDAL HTR2A

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Risperdal

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ARIPIPRAZOLE HTR2A

Interaction Score: 0.22

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Specific Action of the Ligand Partial agonist

PMIDs:
17242925 17265076 14642974 26346901

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
SB-773812 HTR2A

Interaction Score: 0.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
ZIPRASIDONE HTR2A

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
11509214 14728084 17450180 12445705 17848919 12530423 15121646

Sources:
TdgClinicalTrial TEND GuideToPharmacology
METHYSERGIDE HTR2A

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Trial Name -

PMIDs:
10080233 11061982 11720080 10455282 11704657

Sources:
TdgClinicalTrial TEND GuideToPharmacology
THIORIDAZINE HTR2A

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
7898773 8680734 9918563 2866233 2423886

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
ERGOTAMINE HTR2A

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
11752352 8014033 2758221

Sources:
GuideToPharmacology
LOXAPINE HTR2A

Interaction Score: 0.19

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name AZ-004

Novel drug target Established target

Specific Action of the Ligand Inverse agonist

PMIDs:
12664192

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology
PIPAMPERONE HTR2A

Interaction Score: 0.17

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
8935801

Sources:
GuideToPharmacology
MOLINDONE HTR2A

Interaction Score: 0.17

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
2586632

Sources:
GuideToPharmacology
PROMAZINE HTR2A

Interaction Score: 0.17

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12106771 10980325 17016423 17139284 19110200

Sources:
TdgClinicalTrial TEND
PAROXETINE HTR2A

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
11403977 11136637 19361869 18253134 17697394 14514498 23338224 5821956

Sources:
PharmGKB
QUETIAPINE FUMARATE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ZIPRASIDONE HYDROCHLORIDE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL473186 HTR2A

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
ZIPRASIDONE MESYLATE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LURASIDONE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name lurasidone, SM-13496,Latuda

Novel drug target Established target

PMIDs:
23545936

Sources:
TdgClinicalTrial
BUFOTENINE HTR2A

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
PERGOLIDE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
18691132 10641988 18703043 18096760

Sources:
GuideToPharmacology
GLEMANSERIN HTR2A

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
ARIPIPRAZOLE LAUROXIL HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RELENOPRIDE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
VABICASERIN HYDROCHLORIDE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RS-102,221 HTR2A

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
THIOTHIXENE HYDROCHLORIDE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LORCASERIN HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BROLAMFETAMINE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CARPHENAZINE MALEATE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
CABERGOLINE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
20426763 18992242 18691132 10641988

Sources:
GuideToPharmacology
OCAPERIDONE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
TTD
ILOPERIDONE HTR2A

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Novel drug target Established target

PMIDs:
8997630 12861482

Sources:
TdgClinicalTrial ChemblInteractions TTD
SERTINDOLE HTR2A

Interaction Score: 0.14

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Serdolect

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
11594443 7530204 16925508

Sources:
TdgClinicalTrial TEND GuideToPharmacology
OLANZAPINE HTR2A

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

Novel drug target Established target

Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

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

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB
FLUVOXAMINE HTR2A

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19361869 16874005 16205777

Sources:
PharmGKB
QUETIAPINE HTR2A

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
17563257 11132243 12973385 17848919 16038601

Sources:
TdgClinicalTrial TEND GuideToPharmacology
HALOPERIDOL LACTATE HTR2A

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
QUIPAZINE HTR2A

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ZICRONAPINE HTR2A

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CYAMEMAZINE HTR2A

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
HALOPERIDOL DECANOATE HTR2A

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ASENAPINE HTR2A

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Asenapine

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
18308814 10592235 21655346

Sources:
TdgClinicalTrial GuideToPharmacology
MIANSERIN HTR2A

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
11004734

Sources:
TdgClinicalTrial TEND GuideToPharmacology
DOXEPIN HTR2A

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 19179941 309138

Sources:
TdgClinicalTrial
ONDANSETRON HTR2A

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9767524

Sources:
NCI
ANIRACETAM HTR2A

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11412837

Sources:
TTD
RISPERIDONE HTR2A

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Inverse agonist

PMIDs:
11132243 15992090 17316700 15907153 32462699 23859574 19997080 19494443 25943458

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB
CLOZAPINE HTR2A

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
7520908 12973385 15037867 14530903 14751426 14687870 9926100 8916101 24885933

Sources:
TdgClinicalTrial ChemblInteractions NCI TEND GuideToPharmacology PharmGKB
LYSERGIDE HTR2A

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
OLANZAPINE PAMOATE HTR2A

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LOXAPINE HYDROCHLORIDE HTR2A

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CYCLOBENZAPRINE HYDROCHLORIDE HTR2A

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RENZAPRIDE HTR2A

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name renzapride

PMIDs:
None found

Sources:
TdgClinicalTrial
MESULERGINE HTR2A

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
KETANSERIN HTR2A

Interaction Score: 0.09

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
9767524 17031071

Sources:
NCI GuideToPharmacology
TRAZODONE HYDROCHLORIDE HTR2A

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
LISURIDE HTR2A

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
9600588 18691132

Sources:
GuideToPharmacology
THIETHYLPERAZINE HTR2A

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
NEFAZODONE HYDROCHLORIDE HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LOXAPINE SUCCINATE HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESMIRTAZAPINE MALEATE HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRYPTAMINE HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? True

PMIDs:
None found

Sources:
GuideToPharmacology TTD
BIFEPRUNOX HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name bifeprunox, DU127090

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
DROPERIDOL HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
ESCITALOPRAM HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
19365399 24424469

Sources:
PharmGKB
PINDOLOL HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
CHEMBL309760 HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
SPIRAMIDE HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
AGOMELATINE HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CHLORPROMAZINE HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

Specific Action of the Ligand Inverse agonist

PMIDs:
7908055 10821438 8593484

Sources:
ChemblInteractions GuideToPharmacology
TERGURIDE HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Trial Name terguride

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology
AMITRIPTYLINE HTR2A

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name OMS-103HP

Novel drug target Established target

PMIDs:
7855217 19800913

Sources:
TdgClinicalTrial
CITALOPRAM HTR2A

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30221791 23158458 19590397 17671280

Sources:
PharmGKB
TRIMIPRAMINE MALEATE HTR2A

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BROMOCRIPTINE HTR2A

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
18691132 10641988 18703043

Sources:
GuideToPharmacology
MK-212 HTR2A

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
APOMORPHINE HTR2A

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
18691132 15037665

Sources:
GuideToPharmacology
VENLAFAXINE HTR2A

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22006095

Sources:
PharmGKB
FLUPHENAZINE HTR2A

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
17606915

Sources:
GuideToPharmacology
ZOTEPINE HTR2A

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology TTD
PROMAZINE HYDROCHLORIDE HTR2A

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BUPROPION HTR2A

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22947179

Sources:
PharmGKB
DONITRIPTAN HTR2A

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SUMATRIPTAN HTR2A

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25096645

Sources:
PharmGKB
BRL-15,572 HTR2A

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
VORTIOXETINE HTR2A

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
CAPESEROD HTR2A

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
None found

Sources:
GuideToPharmacology
SEROTONIN HTR2A

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? True

Specific Action of the Ligand Full agonist

PMIDs:
7221567

Sources:
GuideToPharmacology
QUINPIROLE HTR2A

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
EFAVIRENZ HTR2A

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23859571

Sources:
PharmGKB
RITANSERIN HTR2A

Interaction Score: 0.04

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
17031071

Sources:
GuideToPharmacology
8-OH-DPAT HTR2A

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
TRIFLUOPERAZINE HYDROCHLORIDE HTR2A

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FLUSPIRILENE HTR2A

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
8935801

Sources:
GuideToPharmacology
METHYLERGONOVINE HTR2A

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
TEDATIOXETINE HTR2A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
ROXINDOLE HTR2A

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
XANOMELINE HTR2A

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
THIORIDAZINE HYDROCHLORIDE HTR2A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PIMOZIDE HTR2A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
CHLORPROMAZINE HYDROCHLORIDE HTR2A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
HALOPERIDOL HTR2A

Interaction Score: 0.02

Interaction Types & Directionality:

other/unknown

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
7520908 12629531

Sources:
ChemblInteractions GuideToPharmacology
SPIPERONE HTR2A

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
METERGOLINE HTR2A

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
DULOXETINE HTR2A

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
PERPHENAZINE HTR2A

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
METITEPINE HTR2A

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
LITHIUM HTR2A

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10758249

Sources:
NCI
PROCHLORPERAZINE HTR2A

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
TRIFLUOPERAZINE HTR2A

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
FLUOXETINE HTR2A

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name NPL-2008, Fluoxetine

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Ensembl: ENSG00000102468
- Version: 101_38
Alternate Names:

HTR2A Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P28223
- Version: 01-August-2011
Alternate Names:

P28223 Uniprot Accession

5HT2A_HUMAN Uniprot Id

HTR2A Gene Symbol

Gene Info:

Target Main Class Receptors

Target Subclass Rhodopsin

Transmembrane Helix Count 7

Publications:
RussLampel: ENSG00000102468
- Version: 26-July-2011
Alternate Names:

HTR2A Display Id

5-HYDROXYTRYPTAMINE 2A RECEPTOR (5-HT-2A) (SEROTONIN RECEPTOR 2A) (5- HT-2). [SOURCE:UNIPROT/SWISSPROT;ACC:P28223] Description

ENSG00000102468 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
HopkinsGroom: P28223
- Version: 11-September-2012
Alternate Names:

3356 Entrez Gene Id

5-HYDROXYTRYPTAMINE RECEPTOR 2A Uniprot Protein Name

HTR2A Uniprot Gene Name

Gene Info:

Human Readable Name G PROTEIN COUPLED RECEPTOR

Interpro Acc IPR000276

Uniprot Status Swiss-Prot

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P28223
- Version: January-2014
Alternate Names:

HTR2A Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
GuideToPharmacology: 3356
- Version: 29-September-2020
Alternate Names:

5293 HUGO Gene ID

5293 HUGO Gene Symbol

5-hydroxytryptamine receptor 2A 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: HTR2A

Version: 18-August-2020

Alternate Names:

PA193 PharmGKB ID

Gene Info:

Publications:

Tiwari AK et al., 2013, Analysis of 34 candidate genes in bupropion and placebo remission., Int J Neuropsychopharmacol

Ujike H et al., 2008, Multiple genetic factors in olanzapine-induced weight gain in schizophrenia patients: a cohort study., J Clin Psychiatry

Angelucci F et al., 2009, Delusion symptoms and response to antipsychotic treatment are associated with the 5-HT2A receptor polymorphism (102T/C) in Alzheimer's disease: a 3-year follow-up longitudinal study., J Alzheimers Dis

TTD: 5-HT 2A receptor

Version: 2020.06.01

Alternate Names:

HTR2A TTD Gene Abbreviation

T32060 TTD Target ID

Gene Info:

Publications:

Guo JD et al., 2009, Bi-directional modulation of bed nucleus of stria terminalis neurons by 5-HT: molecular expression and functional properties of excitatory 5-HT receptor subtypes., Neuroscience

Chen J et al., 2011, Novel ocular antihypertensive compounds in clinical trials., Clin Ophthalmol

NCI: HTR2A

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Serretti et al., Serotonin receptor 2A, 2C, 1A genes and response to lithium prophylaxis in mood disorders., J Psychiatr Res

Kasho et al., 1998, Serotonin enhances the production of type IV collagen by human mesangial cells., Kidney Int.

Arranz et al., 1996, Analysis of a structural polymorphism in the 5-HT2A receptor and clinical response to clozapine., Neurosci. Lett.

HingoraniCasas: ENSG00000102468
- Version: 31-May-2017
Alternate Names:

ENSG00000102468 Gene Symbol

HTR2A Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: HTR2
- Version: chembl_23
Alternate Names:

HTR2 GENE_SYMBOL

HTR2A GENE_SYMBOL

5-hydroxytryptamine receptor 2A UNIPROT

Gene Info:

Publications:
dGene: HTR2A
- Version: 27-Jun-2013
Alternate Names:

3356 Gene ID

5-HT2A dGene Synonym

HTR2 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
GO: HTR2A
- Version: 01-May-2021
Alternate Names:

HTR2 GO Gene Synonym

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:
Pharos: HTR2A
- Version: 01-May-2021
Alternate Names:

5-hydroxytryptamine receptor 2A Gene Name

P28223 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:

Novel drug target	Established target
Trial Name	Pimavanserin
Details of the Assay for Interaction	Ki determined in membrane radioligand binding assay.

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

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

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

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

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

Trial Name	INN-00835, nemifitide
Novel drug target	Established target

Trial Name	esmirtazapine, ORG-4420
Novel drug target	Established target

Specific Action of the Ligand	Partial agonist
Endogenous Drug?	False

Trial Name	AZ-004
Novel drug target	Established target
Specific Action of the Ligand	Inverse agonist

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

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False

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

Trial Name	Serdolect
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

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

Trial Name	Asenapine
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

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

Trial Name	bifeprunox, DU127090
Novel drug target	Established target

Trial Name	NPL-2008, Fluoxetine
Novel drug target	Established target

P28223	Uniprot Accession
5HT2A_HUMAN	Uniprot Id
HTR2A	Gene Symbol

HTR2A Gene Record

HTR2A 3356 Druggable GenomeDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

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

Interaction Info: Novel drug target Established target Trial Name Pimavanserin Details of the Assay for Interaction Ki determined in membrane radioligand binding assay.

PMIDs: 24016069

Sources: TdgClinicalTrial GuideToPharmacology TTD

Interaction Types & Directionality: inverse agonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inverse agonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 20030420

Sources: GuideToPharmacology TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 8884233 12498911 21975349

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inverse agonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 2530096 2975224 1361012 3836113

Sources: TdgClinicalTrial TEND

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

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

PMIDs: 19672037 17031071

Sources: GuideToPharmacology TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 7855217 12873632 10220119 9098663 14520130 10577608 7649970 10435395

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 7520908 7524043 7531353 7542676 11132243 12211096

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 30596390

Sources: TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Pimavanserin

Details of the Assay for Interaction Ki determined in membrane radioligand binding assay.

PMIDs:
24016069

Sources:
TdgClinicalTrial GuideToPharmacology TTD

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor inverse agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor inverse agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name iferanserin ointment

Novel drug target Established target

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
20030420

Sources:
GuideToPharmacology TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8884233 12498911 21975349

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Trial Name volinanserin

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor inverse agonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2530096 2975224 1361012 3836113

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
19672037 17031071

Sources:
GuideToPharmacology TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
7855217 12873632 10220119 9098663 14520130 10577608 7649970 10435395

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name paliperidone ER, paliperidone palmitate

Novel drug target Established target

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
7520908 7524043 7531353 7542676 11132243 12211096

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name INN-00835, nemifitide

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name ITI-007, ITI-722

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

PMIDs:
30596390

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
10821438 8593484

Sources:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name trazodone extended release, DDS-04A,Oleptro

Specific Action of the Ligand Antagonist

PMIDs:
3039120 1365657 10594316 11714900 15610924 7855217 12782915 15614572

Sources:
TdgClinicalTrial TEND GuideToPharmacology

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

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

5293	HUGO Gene ID
5293	HUGO Gene Symbol
5-hydroxytryptamine receptor 2A	HUGO Gene Name

HTR2	GENE_SYMBOL
HTR2A	GENE_SYMBOL
5-hydroxytryptamine receptor 2A	UNIPROT