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
BE0000451
PA193
5-HYDROXYTRYPTAMINE (SEROTONIN) RECEPTOR 2A
6
5-HT<sub>2A</sub> receptor
BE0004881
TTDS00103
5-HYDROXYTRYPTAMINE 2A RECEPTOR
5-HT2A RECEPTOR
SEROTONIN RECEPTOR
5-HYDROXYTRYPTAMINE 2A RECEPTOR (5-HT-2A) (SEROTONIN RECEPTOR 2A) (5- HT-2). [SOURCE:UNIPROT/SWISSPROT;ACC:P28223]
BE0004957
5-HT 2A receptor
T32060

Gene Info:

Target Main Class	Receptors
Target Subclass	Rhodopsin
Transmembrane Helix Count	7
Target Subclass	GPCR
Has Variant Annotation	true
Is VIP	false
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

(13 More Sources)

Gene Categories: Category Details

KINASE
SERINE THREONINE KINASE
DRUG RESISTANCE
G PROTEIN COUPLED RECEPTOR
PHOSPHOLIPASE
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.
Tyson et al., 2004, Are the cognitive effects of atypical antipsychotics influenced by their affinity to 5HT-2A receptors?, Int. J. Neurosci.
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.
Gjerden et al., 2009, Association between the use of anticholinergic antiparkinson drugs and safety and receptor drug-binding profiles of antipsychotic agents., Eur. J. Clin. Pharmacol.
Nyberg et al., 1995, Central D2 receptor occupancy and effects of zuclopenthixol acetate in humans., Int Clin Psychopharmacol
Khalifa, 2003, Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms., Pharmacol. Biochem. Behav.
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.)
Kaumann, 1983, Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors., Naunyn Schmiedebergs Arch. Pharmacol.
Baxter et al., 1994, Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle., Br. J. Pharmacol.
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
Dupont et al., 1996, Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor., Eur. Respir. J.
Dupont et al., 1999, Epinastine (WAL 801CL) inhibits the electrical field stimulation-induced cholinergic contraction in guinea pig and human airways in vitro., Eur. Respir. J.
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
Berger et al., 1996, Trimipramine: a challenge to current concepts on antidepressives., Eur Arch Psychiatry Clin Neurosci
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.
Hayslett et al., 2003, Effects of donepezil on DOI-induced head twitch response in mice: implications for Tourette syndrome., Pharmacol. Biochem. Behav.
Hayslett et al., 2005, Effects of donepezil, nicotine and haloperidol on the central serotonergic system in mice: implications for Tourette's syndrome., Pharmacol. Biochem. Behav.
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
Reimold et al., 2007, Occupancy of dopamine D(1), D (2) and serotonin (2A) receptors in schizophrenic patients treated with flupentixol in comparison with risperidone and haloperidol., Psychopharmacology (Berl.)
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
Newcombe F et al., 1969, Alkaloids of the leaves of Voacanga schweinfurthii Stapf., Planta Med
Foster RH et al., 1997, Paroxetine : a review of its pharmacology and therapeutic potential in the management of panic disorder., CNS Drugs
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
Martin et al., 1982, Ketamine inhibits serotonin uptake in vivo., Neuropharmacology
Fiorella et al., 1995, The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis., Psychopharmacology (Berl.)
Kelley et al., 1997, The role of muscarinic cholinergic receptors in the discriminative stimulus properties of clozapine in rats., Pharmacol. Biochem. Behav.
Bileviciute et al., 1998, Unilateral injection of calcitonin gene-related peptide (CGRP) induces bilateral oedema formation and release of CGRP-like immunoreactivity in the rat hindpaw., Br. 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.
Martinez et al., 1990, A comparison of the effects of chlorpromazine and more selective histamine and 5-hydroxytryptamine antagonists on human IgG synthesis in vitro., Int. J. Immunopharmacol.
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.)
Zanoveli et al., 2005, Chronic imipramine treatment sensitizes 5-HT1A and 5-HT 2 A receptors in the dorsal periaqueductal gray matter: evidence from the elevated T-maze test of anxiety., Behav Pharmacol
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
Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Wander et al., 1986, Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro., Eur. J. Pharmacol.
Contreras et al., Cortical and septal responses to dorsal raphe nucleus stimulation in the rat: long-term clomipramine actions., Bol Estud Med Biol
Sugimoto et al., 2003, The tricyclic antidepressant clomipramine increases plasma glucose levels of mice., J. Pharmacol. Sci.
Trifunović et al., 1996, The effects of clomipramine on the excitatory action of ethanol on dopaminergic neurons of the ventral tegmental area in vitro., J. Pharmacol. Exp. Ther.
Hentall et al., 2000, Correlations between serotonin level and single-cell firing in the rat's nucleus raphe magnus., Neuroscience
Sargent et al., 1998, Clomipramine enhances the cortisol response to 5-HTP: implications for the therapeutic role of 5-HT2 receptors., Psychopharmacology (Berl.)
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
Svartengren et al., 1990, Receptor binding properties of amperozide., Pharmacol. Toxicol.
George et al., 2013, Newer antipsychotics and upcoming molecules for schizophrenia., Eur. J. Clin. Pharmacol.
Green et al., 2004, Focus on levomepromazine., Curr Med Res Opin
Kanerva et al., 1999, Brain 5-HT2A receptor occupancy of deramciclane in humans after a single oral administration--a positron emission tomography study., Psychopharmacology (Berl.)
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.)
Seeman et al., 1997, Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors., Neuropsychopharmacology
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
Cushing et al., 1993, Serotonin-induced contraction in porcine coronary artery: use of ergolines to support vascular 5-hydroxytryptamine2-receptor heterogeneity., J. Pharmacol. Exp. Ther.
Nieto et al., 2000, In vitro effects of 5-hydroxytryptamine and cisapride on the circular smooth muscle of the jejunum of horses., Am. J. Vet. Res.
Beubler et al., 1990, Stimulatory effects of 5-hydroxytryptamine on fluid secretion and transmural potential difference in rat small intestine are mediated by different receptor subtypes., J. Pharm. Pharmacol.
Tiwari AK et al., 2013, Analysis of 34 candidate genes in bupropion and placebo remission., Int J Neuropsychopharmacol
Pälvimäki et al., 1996, Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor., Psychopharmacology (Berl.)
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.
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
Alarcón-de-la-Lastra Romero et al., 1997, Cinitapride protects against ethanol-induced gastric mucosal injury in rats: role of 5-hydroxytryptamine, prostaglandins and sulfhydryl compounds., Pharmacology
Alarcón de la Lastra et al., 1998, Effects of cinitapride on gastric ulceration and secretion in rats., Inflamm. Res.
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.
Bravo L et al., 2019, Monoamines as Drug Targets in Chronic Pain: Focusing on Neuropathic Pain., Front Neurosci
Sánchez et al., 1999, Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding., Cell. Mol. Neurobiol.
Sánchez Martín A et al., 2013, Impact of pharmacogenetics on CNS side effects related to efavirenz., Pharmacogenomics
Beattie et al., 2004, The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo., Br. J. Pharmacol.
McCormack, 2015, Cariprazine: First Global Approval., Drugs
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
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)
Stryjer R et al., 2003, Treatment of neuroleptic-induced akathisia with the 5-HT2A antagonist trazodone., Clin Neuropharmacol
Cargnin S et al., 2014, Combined effect of common gene variants on response to drug withdrawal therapy in medication overuse headache., Eur J Clin Pharmacol
Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr
Maj et al., 1977, Doxepin as a blocker of central serotonin receptors., Pharmakopsychiatr Neuropsychopharmakol
Lohoff FW et al., 2013, Serotonin receptor 2A (HTR2A) gene polymorphism predicts treatment response to venlafaxine XR in generalized anxiety disorder., Pharmacogenomics J
Demirbugen Oz M et al., 2018, The relationship between the serotonin 2A receptor gene -1438A/G and 102T/C polymorphisms and citalopram/sertraline-induced nausea in major depressed patients., Hum Psychopharmacol
Smith RM et al., 2013, Multiple regulatory variants modulate expression of 5-hydroxytryptamine 2A receptors in human cortex., Biol Psychiatry
Illi A et al., 2009, 5-HTR1A, 5-HTR2A, 5-HTR6, TPH1 and TPH2 polymorphisms and major depression., Neuroreport
Paddock S et al., 2007, Association of GRIK4 with outcome of antidepressant treatment in the STAR*D cohort., Am J Psychiatry
Pandey DK et al., 2010, A novel 5-HT(2A) receptor antagonist exhibits antidepressant-like effects in a battery of rodent behavioural assays: approaching early-onset antidepressants., Pharmacol Biochem Behav
Kato M et al., 2006, Effects of the serotonin type 2A, 3A and 3B receptor and the serotonin transporter genes on paroxetine and fluvoxamine efficacy and adverse drug reactions in depressed Japanese patients., Neuropsychobiology
Suzuki Y et al., 2006, Polymorphisms in the 5-hydroxytryptamine 2A receptor and CytochromeP4502D6 genes synergistically predict fluvoxamine-induced side effects in japanese depressed patients., Neuropsychopharmacology
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
Morales P et al., 2017, An Overview on Medicinal Chemistry of Synthetic and Natural Derivatives of Cannabidiol., Front Pharmacol
Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics
Fitzgerald et al., 2000, Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine., Mol. Pharmacol.
Belcheva S et al., 1995, Effects on nociception of the Ca2+ and 5-HT antagonist dotarizine and other 5-HT receptor agonists and antagonists., Acta Physiol Pharmacol Bulg
Farré M et al., 1997, Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration., Methods Find Exp Clin Pharmacol
Kishi T et al., 2013, Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials., CNS Drugs
Tanaka H et al., 1998, Localization and pharmacological characterization of [3H]perospirone-binding sites in rat brain., Gen Pharmacol
Przegaliński E et al., 1979, The central action of pizotifen., Psychopharmacology (Berl)
Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
Jarema M et al., 2011, [Trazodon--the antidepressant: mechanism of action and its position in the treatment of depression]., Psychiatr Pol
Fulton A et al., 1982, Assessment of the antidepressant activity of dothiepin and its metabolites by preclinical tests., J Affect Disord
Abelaira HM et al., 2012, Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats., Pharmacol Biochem Behav

BREXPIPRAZOLE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Trial Name OPC-34712

Publications:

Maeda et al., 2014, Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator., J. Pharmacol. Exp. Ther.
ILOPERIDONE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Novel drug target Established target

Publications:

Kongsamut et al., 1996, Iloperidone binding to human and rat dopamine and 5-HT receptors., Eur. J. Pharmacol.

Hesselink, 2002, Iloperidone (Novartis)., IDrugs
LUMATEPERONE HTR2A

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

Publications:

Kumar B et al., 2018, Lumateperone: a new treatment approach for neuropsychiatric disorders., Drugs Today (Barc)

CHLORPROTHIXENE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

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

Publications:

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.

HALOPERIDOL HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

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

MIANSERIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

FLIBANSERIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Direct Interaction? True

Endogenous Drug? False

Publications:

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.

ASENAPINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Asenapine

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

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.

Citrome, 2011, Role of sublingual asenapine in treatment of schizophrenia., Neuropsychiatr Dis Treat

MESORIDAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

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.

SERTINDOLE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Serdolect

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

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

THIORIDAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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.

PIMAVANSERIN HTR2A

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.

Publications:

Friedman, 2013, Pimavanserin for the treatment of Parkinson's disease psychosis., Expert Opin Pharmacother
BLONANSERIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Deeks ED et al., 2010, Blonanserin: a review of its use in the management of schizophrenia., CNS Drugs

MOLINDONE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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.

THIOTHIXENE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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.

LOXAPINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name AZ-004

Novel drug target Established target

Specific Action of the Ligand Inverse agonist

Publications:

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.)

QUINPIROLE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
AGOMELATINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
METHYLERGONOVINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Publications:
TRAZODONE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Publications:
SB-773812 HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Publications:
TRELANSERIN HTR2A

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

Publications:
IFERANSERIN HTR2A

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

Publications:
MK-212 HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
PRUVANSERIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
CARPHENAZINE MALEATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Publications:
TEDATIOXETINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Publications:
ZOTEPINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:
BROLAMFETAMINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
PIMOZIDE HTR2A

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

Publications:
THIORIDAZINE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
LORCASERIN HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
SPIRAMIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
HALOPERIDOL DECANOATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
THIOTHIXENE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
RS-102,221 HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
CHLORPROMAZINE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Publications:
VABICASERIN HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
PROMAZINE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
RELENOPRIDE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

Publications:
XANOMELINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:
chembl:CHEMBL309760 HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Publications:
CAPESEROD HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

Publications:
ARIPIPRAZOLE LAUROXIL HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
TEMANOGREL HTR2A

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
TERGURIDE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Trial Name terguride

Publications:
NELOTANSERIN HTR2A

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
GLEMANSERIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:
METERGOLINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
LURASIDONE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
MESORIDAZINE BESYLATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
BUFOTENINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
MESULERGINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
SPIPERONE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:
PINDOLOL HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:
SERGOLEXOLE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
TRIMIPRAMINE MALEATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
VORTIOXETINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:
BRL-15,572 HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
AMESERGIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
CYAMEMAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
DROPERIDOL HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Publications:
PIMAVANSERIN TARTRATE HTR2A

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Publications:
CYCLOBENZAPRINE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
ZIPRASIDONE MESYLATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
PERPHENAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
EPLIVANSERIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
LOXAPINE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
TRIFLUOPERAZINE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
QUIPAZINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
8-OH-DPAT HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
TRYPTAMINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? True

Publications:
chembl:CHEMBL473186 HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
ZIPRASIDONE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
DONITRIPTAN HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
TRIFLUOPERAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:
METITEPINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
ESMIRTAZAPINE MALEATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
HALOPERIDOL LACTATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
LOXAPINE SUCCINATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
VOLINANSERIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Trial Name volinanserin

Publications:
OLANZAPINE PAMOATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
DULOXETINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
NEFAZODONE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
ASENAPINE MALEATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
MOLINDONE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
LYSERGIDE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
ROXINDOLE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
QUETIAPINE FUMARATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:

CHLORPROMAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

binder

Interaction Info:

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

Direct Interaction yes

Specific Action of the Ligand Inverse agonist

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.

AMISULPRIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Tyson et al., 2004, Are the cognitive effects of atypical antipsychotics influenced by their affinity to 5HT-2A receptors?, Int. J. Neurosci.

CABERGOLINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:

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

THIOPROPERAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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.

ZUCLOPENTHIXOL HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Gjerden et al., 2009, Association between the use of anticholinergic antiparkinson drugs and safety and receptor drug-binding profiles of antipsychotic agents., Eur. J. Clin. Pharmacol.

Nyberg et al., 1995, Central D2 receptor occupancy and effects of zuclopenthixol acetate in humans., Int Clin Psychopharmacol

Khalifa, 2003, Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms., Pharmacol. Biochem. Behav.

MIDOMAFETAMINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

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.)

YOHIMBINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Kaumann, 1983, Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors., Naunyn Schmiedebergs Arch. Pharmacol.

Baxter et al., 1994, Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle., Br. J. Pharmacol.

CYCLOBENZAPRINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

SEROTONIN HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? True

Specific Action of the Ligand Full agonist

Publications:

Peroutka et al., 1981, Two distinct central serotonin receptors with different physiological functions., Science

EPINASTINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Dupont et al., 1996, Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor., Eur. Respir. J.

Dupont et al., 1999, Epinastine (WAL 801CL) inhibits the electrical field stimulation-induced cholinergic contraction in guinea pig and human airways in vitro., Eur. Respir. J.

TRIMIPRAMINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Berger et al., 1996, Trimipramine: a challenge to current concepts on antidepressives., Eur Arch Psychiatry Clin Neurosci

QUETIAPINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

DONEPEZIL HTR2A

Interaction Types & Directionality:

inducer (activating)

Interaction Info:

Publications:

Hayslett et al., 2003, Effects of donepezil on DOI-induced head twitch response in mice: implications for Tourette syndrome., Pharmacol. Biochem. Behav.

Hayslett et al., 2005, Effects of donepezil, nicotine and haloperidol on the central serotonergic system in mice: implications for Tourette's syndrome., Pharmacol. Biochem. Behav.

FLUPENTIXOL HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Reimold et al., 2007, Occupancy of dopamine D(1), D (2) and serotonin (2A) receptors in schizophrenic patients treated with flupentixol in comparison with risperidone and haloperidol., Psychopharmacology (Berl.)

LISURIDE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Publications:

Egan et al., 1998, Agonist activity of LSD and lisuride at cloned 5HT2A and 5HT2C receptors., Psychopharmacology (Berl.)

Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem

PAROXETINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

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

ROPINIROLE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem

CLOZAPINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Leysen et al., 1994, Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity., J Clin Psychiatry

Goldstein, 1999, Quetiapine fumarate (Seroquel): a new atypical antipsychotic., Drugs Today

Reist et al., 2004, Inter-relationships of intermediate phenotypes for serotonin function, impulsivity, and a 5-HT2A candidate allele: His452Tyr., Mol. Psychiatry

RITANSERIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

inverse agonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

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

ARIPIPRAZOLE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

partial agonist (activating)

Interaction Info:

Direct Interaction yes

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

Specific Action of the Ligand Partial agonist

Publications:

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

MIRTAZAPINE HTR2A

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

Publications:

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

FLUPHENAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Bisson WH et al., 2007, Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs., Proc Natl Acad Sci U S A
KETAMINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Martin et al., 1982, Ketamine inhibits serotonin uptake in vivo., Neuropharmacology

PROMETHAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Fiorella et al., 1995, The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis., Psychopharmacology (Berl.)

Kelley et al., 1997, The role of muscarinic cholinergic receptors in the discriminative stimulus properties of clozapine in rats., Pharmacol. Biochem. Behav.

Bileviciute et al., 1998, Unilateral injection of calcitonin gene-related peptide (CGRP) induces bilateral oedema formation and release of CGRP-like immunoreactivity in the rat hindpaw., Br. J. Pharmacol.

PALIPERIDONE HTR2A

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

Publications:

Leysen et al., 1994, Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity., J Clin Psychiatry

Cohen, Risperidone., Pharmacotherapy

Megens et al., 1994, Survey on the pharmacodynamics of the new antipsychotic risperidone., Psychopharmacology (Berl.)

KETANSERIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

inverse agonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

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

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

NEFAZODONE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

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

IMIPRAMINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Zanoveli et al., 2005, Chronic imipramine treatment sensitizes 5-HT1A and 5-HT 2 A receptors in the dorsal periaqueductal gray matter: evidence from the elevated T-maze test of anxiety., Behav Pharmacol

RISPERIDONE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Inverse agonist

Publications:

Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.

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.

OLANZAPINE HTR2A

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)

Publications:

Maffioletti E et al., 2020, Association study between HTR2A rs6313 polymorphism and early response to risperidone and olanzapine in schizophrenia patients., Drug Dev Res

Salloum NC et al., 2014, Towards the clinical implementation of pharmacogenetics in bipolar disorder., BMC Med

Laika B et al., 2010, Pharmacogenetics and olanzapine treatment: CYP1A2*1F and serotonergic polymorphisms influence therapeutic outcome., Pharmacogenomics J

SARPOGRELATE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

inverse agonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

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

PROMAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

METHYSERGIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Trial Name -

Publications:

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.

BROMOCRIPTINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Publications:

Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem

Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy

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.

APOMORPHINE HTR2A

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem

LeWitt PA, 2004, Subcutaneously administered apomorphine: pharmacokinetics and metabolism., Neurology

PERGOLIDE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:

Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem

Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy

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.

BUTRIPTYLINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.

Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.

Wander et al., 1986, Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro., Eur. J. Pharmacol.

CLOMIPRAMINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Contreras et al., Cortical and septal responses to dorsal raphe nucleus stimulation in the rat: long-term clomipramine actions., Bol Estud Med Biol

Sugimoto et al., 2003, The tricyclic antidepressant clomipramine increases plasma glucose levels of mice., J. Pharmacol. Sci.

Trifunović et al., 1996, The effects of clomipramine on the excitatory action of ethanol on dopaminergic neurons of the ventral tegmental area in vitro., J. Pharmacol. Exp. Ther.

MINAPRINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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.

AMPEROZIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Svartengren et al., 1990, Receptor binding properties of amperozide., Pharmacol. Toxicol.
LURASIDONE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name lurasidone, SM-13496,Latuda

Novel drug target Established target

Publications:

George et al., 2013, Newer antipsychotics and upcoming molecules for schizophrenia., Eur. J. Clin. Pharmacol.
LEVOMEPROMAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Green et al., 2004, Focus on levomepromazine., Curr Med Res Opin

PIPOTIAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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.

DERAMCICLANE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Kanerva et al., 1999, Brain 5-HT2A receptor occupancy of deramciclane in humans after a single oral administration--a positron emission tomography study., Psychopharmacology (Berl.)
MAPROTILINE HTR2A

Interaction Types & Directionality:

binder

Interaction Info:

Publications:

Peroutka et al., 1981, Two distinct central serotonin receptors with different physiological functions., Science

ESCITALOPRAM HTR2A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

ERGOTAMINE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

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.

FLUSPIRILENE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Schotte et al., 1996, Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding., Psychopharmacology (Berl.)

PROPIOMAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

Adolph O et al., 2012, Promethazine inhibits NMDA-induced currents - new pharmacological aspects of an old drug., Neuropharmacology

CISAPRIDE HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Cushing et al., 1993, Serotonin-induced contraction in porcine coronary artery: use of ergolines to support vascular 5-hydroxytryptamine2-receptor heterogeneity., J. Pharmacol. Exp. Ther.

Nieto et al., 2000, In vitro effects of 5-hydroxytryptamine and cisapride on the circular smooth muscle of the jejunum of horses., Am. J. Vet. Res.

Beubler et al., 1990, Stimulatory effects of 5-hydroxytryptamine on fluid secretion and transmural potential difference in rat small intestine are mediated by different receptor subtypes., J. Pharm. Pharmacol.

AMOXAPINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Pälvimäki et al., 1996, Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor., Psychopharmacology (Berl.)

ZIPRASIDONE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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.

CYPROHEPTADINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

CINITAPRIDE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Alarcón-de-la-Lastra Romero et al., 1997, Cinitapride protects against ethanol-induced gastric mucosal injury in rats: role of 5-hydroxytryptamine, prostaglandins and sulfhydryl compounds., Pharmacology

Alarcón de la Lastra et al., 1998, Effects of cinitapride on gastric ulceration and secretion in rats., Inflamm. Res.

ESMIRTAZAPINE HTR2A

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Trial Name esmirtazapine, ORG-4420

Novel drug target Established target

Publications:

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.

NORTRIPTYLINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Bravo L et al., 2019, Monoamines as Drug Targets in Chronic Pain: Focusing on Neuropathic Pain., Front Neurosci

Sánchez et al., 1999, Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding., Cell. Mol. Neurobiol.

TEGASEROD HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Beattie et al., 2004, The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo., Br. J. Pharmacol.

ACEPROMAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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.

CARIPRAZINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

McCormack, 2015, Cariprazine: First Global Approval., Drugs

TRAZODONE HTR2A

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

Publications:

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.

DOXEPIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

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

AMITRIPTYLINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name OMS-103HP

Novel drug target Established target

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Pandey DK et al., 2010, A novel 5-HT(2A) receptor antagonist exhibits antidepressant-like effects in a battery of rodent behavioural assays: approaching early-onset antidepressants., Pharmacol Biochem Behav

DESIPRAMINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
PIPAMPERONE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Schotte et al., 1996, Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding., Psychopharmacology (Berl.)
ZOLMITRIPTAN HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

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

CANNABIDIOL HTR2A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Morales P et al., 2017, An Overview on Medicinal Chemistry of Synthetic and Natural Derivatives of Cannabidiol., Front Pharmacol

Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics

ETOPERIDONE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

PEROSPIRONE HTR2A

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Publications:

Kishi T et al., 2013, Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials., CNS Drugs

Tanaka H et al., 1998, Localization and pharmacological characterization of [3H]perospirone-binding sites in rat brain., Gen Pharmacol

PIZOTYLINE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Przegaliński E et al., 1979, The central action of pizotifen., Psychopharmacology (Berl)

Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
LORPIPRAZOLE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Jarema M et al., 2011, [Trazodon--the antidepressant: mechanism of action and its position in the treatment of depression]., Psychiatr Pol
DOTHIEPIN HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Fulton A et al., 1982, Assessment of the antidepressant activity of dothiepin and its metabolites by preclinical tests., J Affect Disord
LAMOTRIGINE HTR2A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Abelaira HM et al., 2012, Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats., Pharmacol Biochem Behav
NEMIFITIDE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name INN-00835, nemifitide

Novel drug target Established target

Publications:
THIETHYLPERAZINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
RISPERDAL HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Risperdal

Novel drug target Established target

Publications:
FLUOXETINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name NPL-2008, Fluoxetine

Novel drug target Established target

Publications:
RENZAPRIDE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name renzapride

Publications:
BIFEPRUNOX HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name bifeprunox, DU127090

Novel drug target Established target

Publications:
OCAPERIDONE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
LITHIUM HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Serretti et al., Serotonin receptor 2A, 2C, 1A genes and response to lithium prophylaxis in mood disorders., J Psychiatr Res
ANIRACETAM HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Nakamura et al., 2001, Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism., Eur. J. Pharmacol.
ONDANSETRON HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Kasho et al., 1998, Serotonin enhances the production of type IV collagen by human mesangial cells., Kidney Int.
REMOXIPRIDE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Seeman et al., 1997, Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors., Neuropsychopharmacology
BUPROPION HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Tiwari AK et al., 2013, Analysis of 34 candidate genes in bupropion and placebo remission., Int J Neuropsychopharmacol
PRAMIPEXOLE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem

Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy
EFAVIRENZ HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sánchez Martín A et al., 2013, Impact of pharmacogenetics on CNS side effects related to efavirenz., Pharmacogenomics
SUMATRIPTAN HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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
VENLAFAXINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Lohoff FW et al., 2013, Serotonin receptor 2A (HTR2A) gene polymorphism predicts treatment response to venlafaxine XR in generalized anxiety disorder., Pharmacogenomics J

CITALOPRAM HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Demirbugen Oz M et al., 2018, The relationship between the serotonin 2A receptor gene -1438A/G and 102T/C polymorphisms and citalopram/sertraline-induced nausea in major depressed patients., Hum Psychopharmacol

Smith RM et al., 2013, Multiple regulatory variants modulate expression of 5-hydroxytryptamine 2A receptors in human cortex., Biol Psychiatry

Illi A et al., 2009, 5-HTR1A, 5-HTR2A, 5-HTR6, TPH1 and TPH2 polymorphisms and major depression., Neuroreport

FLUVOXAMINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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

Kato M et al., 2006, Effects of the serotonin type 2A, 3A and 3B receptor and the serotonin transporter genes on paroxetine and fluvoxamine efficacy and adverse drug reactions in depressed Japanese patients., Neuropsychobiology

Suzuki Y et al., 2006, Polymorphisms in the 5-hydroxytryptamine 2A receptor and CytochromeP4502D6 genes synergistically predict fluvoxamine-induced side effects in japanese depressed patients., Neuropsychopharmacology

FENFLURAMINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Fitzgerald et al., 2000, Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine., Mol. Pharmacol.
NABIXIMOLS HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics

DOTARIZINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Belcheva S et al., 1995, Effects on nociception of the Ca2+ and 5-HT antagonist dotarizine and other 5-HT receptor agonists and antagonists., Acta Physiol Pharmacol Bulg

Farré M et al., 1997, Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration., Methods Find Exp Clin Pharmacol

DIHYDROERGOTAMINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PHENYLPIPERAZINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ISOCLOZAPINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
BARETTIN HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL403550 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL180010 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PHENETHYLAMINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DOM HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL77880 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL407909 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TRYPTOLINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL201930 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL76474 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
BL-1020 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CINANSERIN HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL463249 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ZICRONAPINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
NORFLUOXETINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PSILOCIN HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL431298 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ABAPERIDONE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
5-METHOXYTRYPTAMINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
APLYSINOPSIN HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
5-MEO-DMT HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PROCHLORPERAZINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL519240 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL571858 HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
FLUANISONE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ALTANSERIN HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CHLOROPHENYLPIPERAZINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ETISULERGINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MESCALINE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ROLUPERIDONE HYDROCHLORIDE HTR2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000102468
- Version: 101_38
Alternate Names:

HTR2A Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

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

P28223 Uniprot Accession

5HT2A_HUMAN Uniprot Id

HTR2A Gene Symbol

Gene Info:

Target Main Class Receptors

Target Subclass Rhodopsin

Transmembrane Helix Count 7

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

HTR2A Display Id

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

ENSG00000102468 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

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

3356 Entrez Gene Id

5-HYDROXYTRYPTAMINE RECEPTOR 2A Uniprot Protein Name

HTR2A Uniprot Gene Name

Gene Info:

Human Readable Name G PROTEIN COUPLED RECEPTOR

Interpro Acc IPR000276

Uniprot Status Swiss-Prot

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

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

HTR2A Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:

PharmGKB: HTR2A

Version: 18-August-2020

Alternate Names:

PA193 PharmGKB ID

Gene Info:

Publications:

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

Thomas P et al., 2008, Correlates of response to Olanzapine in a North Indian Schizophrenia sample., Psychiatry Res

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

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

Vanover KE et al., 2010, Role of 5-HT2A receptor antagonists in the treatment of insomnia., Nat Sci Sleep

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

DrugBank: BE0000451

Version: 5.1.7

Alternate Names:

HTR2A DrugBank Gene Name

P28223 UniProt Accession

3356 Entrez Gene Id

Gene Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

Stahl et al., 2003, The psychopharmacology of ziprasidone: receptor-binding properties and real-world psychiatric practice., J Clin Psychiatry

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.

DrugBank: BE0004881
- Version: 5.1.7
Alternate Names:

HTR2A DrugBank Gene Name

P28223 UniProt Accession

3356 Entrez Gene Id

Gene Info:

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.

DrugBank: BE0004957

Version: 5.1.7

Alternate Names:

HTR2A DrugBank Gene Name

P28223 UniProt Accession

3356 Entrez Gene Id

Gene Info:

Publications:

Martin et al., 1982, Ketamine inhibits serotonin uptake in vivo., Neuropharmacology

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.

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:
GuideToPharmacologyInteractions: ENSG00000102468
- Version: 20-July-2020
Alternate Names:

5-HT<sub>2A</sub> receptor GuideToPharmacology Name

P28223 UniProtKB ID

Gene Info:

Publications:
Pharos: HTR2A
- Version: 03-September-2020
Alternate Names:

5-hydroxytryptamine receptor 2A Gene Name

P28223 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
GO: HTR2A
- Version: 05-September-2020
Alternate Names:

HTR2 GO Gene Synonym

Gene Info:

Gene Categories:

DRUG RESISTANCE, G PROTEIN COUPLED RECEPTOR

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:

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

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

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

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

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

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

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False

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

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

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

Specific Action of the Ligand	Partial agonist
Endogenous Drug?	False
Trial Name	terguride

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

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

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

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

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

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

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

Trial Name	bifeprunox, DU127090
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: antagonist (inhibitory)

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

Publications: Maeda et al., 2014, Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications: Kongsamut et al., 1996, Iloperidone binding to human and rat dopamine and 5-HT receptors., Eur. J. Pharmacol. Hesselink, 2002, Iloperidone (Novartis)., IDrugs

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

Publications: Kumar B et al., 2018, Lumateperone: a new treatment approach for neuropsychiatric disorders., Drugs Today (Barc)

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications: 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.

Interaction Types & Directionality: antagonist (inhibitory)

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

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications: 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

Interaction Types & Directionality: antagonist (inhibitory)

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

Interaction Types & Directionality: antagonist (inhibitory)

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

Interaction Types & Directionality: antagonist (inhibitory)

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

Interaction Types & Directionality: antagonist (inhibitory)

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

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.

Publications: Friedman, 2013, Pimavanserin for the treatment of Parkinson's disease psychosis., Expert Opin Pharmacother

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications: Deeks ED et al., 2010, Blonanserin: a review of its use in the management of schizophrenia., CNS Drugs

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications: 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.

Interaction Types & Directionality: antagonist (inhibitory)

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

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications: 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.)

Interaction Types & Directionality: agonist (activating)

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

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality: agonist (activating)

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

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

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

Publications:

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

Publications:

Interaction Types & Directionality: agonist (activating)

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

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Trial Name OPC-34712

Publications:

Maeda et al., 2014, Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Novel drug target Established target

Publications:

Kongsamut et al., 1996, Iloperidone binding to human and rat dopamine and 5-HT receptors., Eur. J. Pharmacol.

Hesselink, 2002, Iloperidone (Novartis)., IDrugs

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

Publications:

Kumar B et al., 2018, Lumateperone: a new treatment approach for neuropsychiatric disorders., Drugs Today (Barc)

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Direct Interaction? True

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Asenapine

Novel drug target Established target

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Serdolect

Novel drug target Established target

Specific Action of the Ligand Antagonist

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.

Publications:

Friedman, 2013, Pimavanserin for the treatment of Parkinson's disease psychosis., Expert Opin Pharmacother

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Deeks ED et al., 2010, Blonanserin: a review of its use in the management of schizophrenia., CNS Drugs

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name AZ-004

Novel drug target Established target

Specific Action of the Ligand Inverse agonist

Publications:

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.)

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

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

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

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

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

HTR2A	DrugBank Gene Name
P28223	UniProt Accession
3356	Entrez Gene Id

HTR2	GENE_SYMBOL
HTR2A	GENE_SYMBOL
5-hydroxytryptamine receptor 2A	UNIPROT

5-HT<sub>2A</sub> receptor	GuideToPharmacology Name
P28223	UniProtKB ID