DGIdb - HTR2C Gene Record

HTR2C 3358 Druggable Genome

Alternate Names:

3358
5-HYDROXYTRYPTAMINE RECEPTOR 2C
HTR2C
5-HT1C
5-HT2C
5-HTR2C
5HTR2C
HTR1C
312861
5295
ENSG00000147246
OTTHUMG00000022226
5-HT-2C
Serotonin receptor 2C
5-HT-1C
5-hydroxytryptamine receptor 1C
P28335
5HT2C_HUMAN
PA194
5-HYDROXYTRYPTAMINE 2C RECEPTOR (5-HT-2C) (SEROTONIN RECEPTOR 2C) (5- HT2C) (5-HTR2C) (5HT-1C). [SOURCE:UNIPROT/SWISSPROT;ACC:P28335]
5-HT 2C receptor
T83813

Gene Info:

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

(7 More Sources)

Gene Categories: Category Details

KINASE
G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Opgen-Rhein C et al., 2010, Association of HTR2C, but not LEP or INSIG2, genes with antipsychotic-induced weight gain in a German sample., Pharmacogenomics
Brasch-Andersen C et al., 2011, A candidate gene study of serotonergic pathway genes and pain relief during treatment with escitalopram in patients with neuropathic pain shows significant association to serotonin receptor2C (HTR2C)., Eur J Clin Pharmacol
Sanchez C et al., 2014, A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike?, Int Clin Psychopharmacol
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
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
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
Johnson et al., 2003, An investigation of the 5-HT2C receptor gene as a migraine candidate gene., Am. J. Med. Genet. B Neuropsychiatr. Genet.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.
Wood et al., 2006, Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade., CNS Neurol Disord Drug Targets
Sánchez et al., 2000, In-vivo assessment of 5-HT2A and 5-HT2C antagonistic properties of newer antipsychotics., Behav Pharmacol
Seeger et al., 1995, Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity., J. Pharmacol. Exp. Ther.
Stahl et al., 2003, The psychopharmacology of ziprasidone: receptor-binding properties and real-world psychiatric practice., J Clin Psychiatry
Cates ME, 2003, Ziprasidone--not an option for serotonin syndrome., CMAJ
Millan et al., 2005, Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade., Psychopharmacology (Berl.)
Herrick-Davis et al., 2000, Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors., J. Pharmacol. Exp. Ther.
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
Maj et al., 1977, Doxepin as a blocker of central serotonin receptors., Pharmakopsychiatr Neuropsychopharmakol
Navailles et al., 2006, Clozapine and haloperidol differentially alter the constitutive activity of central serotonin2C receptors in vivo., Biol. Psychiatry
Sodhi et al., 2005, A rapid new assay to detect RNA editing reveals antipsychotic-induced changes in serotonin-2C transcripts., Mol. Pharmacol.
Ma X et al., 2014, HTR2C polymorphisms, olanzapine-induced weight gain and antipsychotic-induced metabolic syndrome in schizophrenia patients: a meta-analysis., Int J Psychiatry Clin Pract
Houston JP et al., 2012, Pharmacogenomic associations with weight gain in olanzapine treatment of patients without schizophrenia., J Clin Psychiatry
Sicard MN et al., 2010, Polymorphisms of the HTR2C gene and antipsychotic-induced weight gain: an update and meta-analysis., Pharmacogenomics
Risselada AJ et al., 2012, Association between HTR2C gene polymorphisms and the metabolic syndrome in patients using antipsychotics: a replication study., Pharmacogenomics J
Godlewska BR et al., 2009, Olanzapine-induced weight gain is associated with the -759C/T and -697G/C polymorphisms of the HTR2C gene., Pharmacogenomics J
Mulder H et al., 2009, HTR2C gene polymorphisms and the metabolic syndrome in patients with schizophrenia: a replication study., J Clin Psychopharmacol
Mulder H et al., 2007, The association between HTR2C gene polymorphisms and the metabolic syndrome in patients with schizophrenia., J Clin Psychopharmacol
Mulder H et al., 2007, The association between HTR2C polymorphisms and obesity in psychiatric patients using antipsychotics: a cross-sectional study., Pharmacogenomics J
Horishita et al., 2006, The tramadol metabolite, O-desmethyl tramadol, inhibits 5-hydroxytryptamine type 2C receptors expressed in Xenopus Oocytes., Pharmacology
Ogata et al., 2004, The inhibitory effects of tramadol on 5-hydroxytryptamine type 2C receptors expressed in Xenopus oocytes., Anesth. Analg.
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.
Zhang JP et al., 2016, Pharmacogenetic Associations of Antipsychotic Drug-Related Weight Gain: A Systematic Review and Meta-analysis., Schizophr Bull
Dos Santos-Júnior A et al., 2016, Pharmacogenetics of Risperidone and Cardiovascular Risk in Children and Adolescents., Int J Endocrinol
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
Ujike H et al., 2008, Multiple genetic factors in olanzapine-induced weight gain in schizophrenia patients: a cohort study., J Clin Psychiatry
De Luca V et al., 2007, HTR2C haplotypes and antipsychotics-induced weight gain: X-linked multimarker analysis., Hum Psychopharmacol
Corena-McLeod M, 2015, Comparative Pharmacology of Risperidone and Paliperidone., Drugs R D
Jandacek, 2005, APD-356 (Arena)., Curr Opin Investig Drugs
Halford, 2006, Obesity drugs in clinical development., Curr Opin Investig Drugs
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.
Benelli et al., 2004, Influence of mirtazapine on the sexual behavior of male rats., Psychopharmacology (Berl.)
Millan, Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies., Therapie
Millan et al., 2000, Mirtazapine enhances frontocortical dopaminergic and corticolimbic adrenergic, but not serotonergic, transmission by blockade of alpha2-adrenergic and serotonin2C receptors: a comparison with citalopram., Eur. J. Neurosci.
Meert et al., 1997, Antagonism of meta-chlorophenylpiperazine-induced inhibition of exploratory activity in an emergence procedure, the open field test, in rats., Behav Pharmacol
Dekeyne et al., 2001, Following long-term training with citalopram, both mirtazapine and mianserin block its discriminative stimulus properties in rats., Psychopharmacology (Berl.)
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
Theisen et al., 2007, No evidence for binding of clozapine, olanzapine and/or haloperidol to selected receptors involved in body weight regulation., Pharmacogenomics J.
Overstreet et al., 2007, Drug challenges reveal differences in mediation of stress facilitation of voluntary alcohol drinking and withdrawal-induced anxiety in alcohol-preferring P rats., Alcohol. Clin. Exp. Res.
Bymaster et al., 1999, Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro., Schizophr. Res.
Zhang et al., 2006, Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoforms., Biochem. Pharmacol.
Hertel, 2006, Comparing sertindole to other new generation antipsychotics on preferential dopamine output in limbic versus striatal projection regions: mechanism of action., Synapse
Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
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.)
Lindström et al., 2006, Sertindole: efficacy and safety in schizophrenia., Expert Opin Pharmacother
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.
Fiorella et al., 1995, The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of m-chlorophenylpiperazine., Psychopharmacology (Berl.)
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.
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)
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.)
Porcelli S et al., 2016, Possible biomarkers modulating haloperidol efficacy and/or tolerability., Pharmacogenomics
Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

LORCASERIN HTR2C

Interaction Score: 4.95

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Lorcaserin

PMIDs:
16259227 16625817

Sources:
TdgClinicalTrial TTD
LORCASERIN HYDROCHLORIDE HTR2C

Interaction Score: 1.24

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MINAPRINE HTR2C

Interaction Score: 1.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
2975224 1361012 17016423 17139284

Sources:
TdgClinicalTrial TEND
CHLORPROTHIXENE HTR2C

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial ChemblInteractions TEND
MIDOMAFETAMINE HTR2C

Interaction Score: 0.74

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
7824160 2871581

Sources:
TTD
VABICASERIN HTR2C

Interaction Score: 0.62

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PUERARIN HTR2C

Interaction Score: 0.62

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
METHYSERGIDE HTR2C

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12555241 11752352

Sources:
TdgClinicalTrial TEND TTD
PROPIOMAZINE HTR2C

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284 19110200 22507664 12678691

Sources:
TdgClinicalTrial TEND
MIRTAZAPINE HTR2C

Interaction Score: 0.59

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
14615872 16433010 10762339 9832994 11271412 11752352

Sources:
ChemblInteractions TEND TTD
TRAZODONE HTR2C

Interaction Score: 0.57

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

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

Novel drug target Established target

PMIDs:
3039120 7659770 1365657 10594316 15614572

Sources:
TdgClinicalTrial
AGOMELATINE HTR2C

Interaction Score: 0.49

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name agomelatine, AGO178C, S-20098,Valdoxan, Thymanax

Novel drug target Established target

PMIDs:
15289999

Sources:
TdgClinicalTrial
ZIPRASIDONE HTR2C

Interaction Score: 0.48

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
11132243 16918396 11103883 7562537 14728084 14638642

Sources:
TEND
OLANZAPINE HTR2C

Interaction Score: 0.48

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

PMIDs:
16983399 16918396 17624999 10227113 11752352 16336943 16952163 22967772 25152019 19142101 17702092 21121776 19193342 17632216 19997080 20680028 20504252 26880915 27217270 19434072 17016522 25032030

Sources:
TdgClinicalTrial ChemblInteractions TEND PharmGKB
SERTINDOLE HTR2C

Interaction Score: 0.45

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Serdolect

PMIDs:
11594443 16925508

Sources:
TdgClinicalTrial TEND
ZIPRASIDONE MESYLATE HTR2C

Interaction Score: 0.41

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
QUETIAPINE FUMARATE HTR2C

Interaction Score: 0.41

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VABICASERIN HYDROCHLORIDE HTR2C

Interaction Score: 0.41

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CARPHENAZINE MALEATE HTR2C

Interaction Score: 0.41

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ZIPRASIDONE HYDROCHLORIDE HTR2C

Interaction Score: 0.41

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ELTOPRAZINE HTR2C

Interaction Score: 0.41

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
LOXAPINE HTR2C

Interaction Score: 0.41

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
10991983

Sources:
ChemblInteractions
NEFAZODONE HTR2C

Interaction Score: 0.37

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
16433010 11752352

Sources:
TTD
MIANSERIN HTR2C

Interaction Score: 0.37

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11004734

Sources:
TdgClinicalTrial TEND
PROMAZINE HTR2C

Interaction Score: 0.36

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 19110200

Sources:
TdgClinicalTrial TEND
RISPERIDONE HTR2C

Interaction Score: 0.36

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
7898773 11132243 27217270 26880915 25152019 22967772 20680028 20504252 19997080 19193342 19142101 17702092 17632216 25943458

Sources:
ChemblInteractions PharmGKB
TRAMADOL HTR2C

Interaction Score: 0.34

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name tramadol,Tridural, Ryzolt

Trial Name tramadol hydrochloride,Ultram

Trial Name tramadol extended-release,Raliva ER

PMIDs:
16679816 15105221

Sources:
TdgClinicalTrial TEND TTD
METHIXENE HYDROCHLORIDE HTR2C

Interaction Score: 0.31

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
CLOZAPINE HTR2C

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16182256 15917433 25152019 22967772 21121776 20680028 20504252 19434072 19142101 17632216 17016522

Sources:
TdgClinicalTrial TEND PharmGKB
TEDATIOXETINE HTR2C

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Lu AA24530

Novel drug target Established target

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD
QUETIAPINE HTR2C

Interaction Score: 0.27

Interaction Types & Directionality:

ligand

antagonist (inhibitory)

Interaction Info:

Trial Name Seroquel

Novel drug target Established target

PMIDs:
11132243 17848919 20504252

Sources:
TdgClinicalTrial TEND PharmGKB
ASENAPINE HTR2C

Interaction Score: 0.27

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Asenapine

Novel drug target Established target

PMIDs:
18308814 10592235 21655346

Sources:
TdgClinicalTrial
AMISULPRIDE HTR2C

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20504252

Sources:
PharmGKB
RENZAPRIDE HTR2C

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name renzapride

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
CYCLOBENZAPRINE HYDROCHLORIDE HTR2C

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
LOXAPINE HYDROCHLORIDE HTR2C

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OLANZAPINE PAMOATE HTR2C

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
TRAZODONE HYDROCHLORIDE HTR2C

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
THIETHYLPERAZINE HTR2C

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
LOXAPINE SUCCINATE HTR2C

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DOXEPIN HTR2C

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 309138

Sources:
TdgClinicalTrial
NEFAZODONE HYDROCHLORIDE HTR2C

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
ESMIRTAZAPINE MALEATE HTR2C

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BIFEPRUNOX HTR2C

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name bifeprunox, DU127090

PMIDs:
None found

Sources:
TdgClinicalTrial
ESCITALOPRAM HTR2C

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
21614492 24424469

Sources:
PharmGKB
TRIMIPRAMINE MALEATE HTR2C

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRIFLUOPERAZINE HYDROCHLORIDE HTR2C

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
THIORIDAZINE HTR2C

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
THIORIDAZINE HYDROCHLORIDE HTR2C

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOPERIDOL HTR2C

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27023437 12629531

Sources:
PharmGKB

Ensembl: ENSG00000147246
- Version: 101_38
Alternate Names:

HTR2C Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P28335
- Version: January-2014
Alternate Names:

HTR2C Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
HopkinsGroom: P28335
- Version: 11-September-2012
Alternate Names:

ENSG00000147246 Ensembl Gene Id

5HT2C_HUMAN Uniprot Id

P28335 Uniprot Accession

Gene Info:

Uniprot Evidence 1: Evidence at protein level

Interpro Short Name 7TM_GPCR_Rhodpsn

Human Readable Name DRUGGABLE GENOME

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P28335
- Version: 01-August-2011
Alternate Names:

ENSG00000147246 Ensembl Gene Id

3358 Entrez Gene Id

P28335 Uniprot Accession

Gene Info:

Target Subclass GPCR

Target Main Class Receptors

Target Subclass Rhodopsin

Publications:

RussLampel: ENSG00000147246

Version: 26-July-2011

Alternate Names:

5-HYDROXYTRYPTAMINE 2C RECEPTOR (5-HT-2C) (SEROTONIN RECEPTOR 2C) (5- HT2C) (5-HTR2C) (5HT-1C). [SOURCE:UNIPROT/SWISSPROT;ACC:P28335] Description

HTR2C Display Id

ENSG00000147246 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

PharmGKB: HTR2C

Version: 18-August-2020

Alternate Names:

PA194 PharmGKB ID

Gene Info:

Publications:

Opgen-Rhein C et al., 2010, Association of HTR2C, but not LEP or INSIG2, genes with antipsychotic-induced weight gain in a German sample., Pharmacogenomics

Brasch-Andersen C et al., 2011, A candidate gene study of serotonergic pathway genes and pain relief during treatment with escitalopram in patients with neuropathic pain shows significant association to serotonin receptor2C (HTR2C)., Eur J Clin Pharmacol

Houston JP et al., 2012, Pharmacogenomic associations with weight gain in olanzapine treatment of patients without schizophrenia., J Clin Psychiatry

TTD: 5-HT 2C receptor
- Version: 2020.06.01
Alternate Names:

HTR2C TTD Gene Abbreviation

T83813 TTD Target ID

Gene Info:

Publications:

Garfield AS et al., 2009, Pharmacological targeting of the serotonergic system for the treatment of obesity., J Physiol
ChemblInteractions: HTR1C
- Version: chembl_23
Alternate Names:

HTR1C GENE_SYMBOL

HTR2C GENE_SYMBOL

5-hydroxytryptamine receptor 2C UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000147246
- Version: 31-May-2017
Alternate Names:

ENSG00000147246 Gene Symbol

HTR2C Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
dGene: HTR2C
- Version: 27-Jun-2013
Alternate Names:

3358 Gene ID

5-HT2C dGene Synonym

5-HTR2C dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
Pharos: HTR2C
- Version: 01-February-2022
Alternate Names:

5-hydroxytryptamine receptor 2C Gene Name

P28335 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:

Mechanism of Interaction	Serotonin 2c (5-HT2c) receptor agonist
Direct Interaction	yes

Novel drug target	Established target
Trial Name	-
Mechanism of Interaction	Serotonin 2c (5-HT2c) receptor antagonist

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

Trial Name	agomelatine, AGO178C, S-20098,Valdoxan, Thymanax
Novel drug target	Established target

Trial Name	tramadol,Tridural, Ryzolt
Trial Name	tramadol hydrochloride,Ultram
Trial Name	tramadol extended-release,Raliva ER

Trial Name	Lu AA24530
Novel drug target	Established target
Mechanism of Interaction	Serotonin 2c (5-HT2c) receptor antagonist

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

ENSG00000147246	Ensembl Gene Id
5HT2C_HUMAN	Uniprot Id
P28335	Uniprot Accession

5-HYDROXYTRYPTAMINE 2C RECEPTOR (5-HT-2C) (SEROTONIN RECEPTOR 2C) (5- HT2C) (5-HTR2C) (5HT-1C). [SOURCE:UNIPROT/SWISSPROT;ACC:P28335]	Description
HTR2C	Display Id
ENSG00000147246	Ensembl Gene Id

HTR1C	GENE_SYMBOL
HTR2C	GENE_SYMBOL
5-hydroxytryptamine receptor 2C	UNIPROT

agonist (activating)
antagonist (inhibitory)

HTR2C Gene Record

HTR2C 3358 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name Lorcaserin

PMIDs: 16259227 16625817

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 2c (5-HT2c) receptor agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 2975224 1361012 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name - Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 7824160 2871581

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 12555241 11752352

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 17016423 17139284 19110200 22507664 12678691

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist Direct Interaction yes

PMIDs: 14615872 16433010 10762339 9832994 11271412 11752352

Sources: ChemblInteractions TEND TTD

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

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

PMIDs: 3039120 7659770 1365657 10594316 15614572

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name agomelatine, AGO178C, S-20098,Valdoxan, Thymanax Novel drug target Established target

PMIDs: 15289999

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 11132243 16918396 11103883 7562537 14728084 14638642

Sources: TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist Direct Interaction yes Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

PMIDs: 16983399 16918396 17624999 10227113 11752352 16336943 16952163 22967772 25152019 19142101 17702092 21121776 19193342 17632216 19997080 20680028 20504252 26880915 27217270 19434072 17016522 25032030

Sources: TdgClinicalTrial ChemblInteractions TEND PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name Serdolect

PMIDs: 11594443 16925508

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 2c (5-HT2c) receptor agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Lorcaserin

PMIDs:
16259227 16625817

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
2975224 1361012 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

agonist (activating)

PMIDs:
7824160 2871581

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12555241 11752352

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284 19110200 22507664 12678691

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
14615872 16433010 10762339 9832994 11271412 11752352

Sources:
ChemblInteractions TEND TTD

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

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

Novel drug target Established target

PMIDs:
3039120 7659770 1365657 10594316 15614572

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name agomelatine, AGO178C, S-20098,Valdoxan, Thymanax

Novel drug target Established target

PMIDs:
15289999

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
11132243 16918396 11103883 7562537 14728084 14638642

Sources:
TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

PMIDs:
16983399 16918396 17624999 10227113 11752352 16336943 16952163 22967772 25152019 19142101 17702092 21121776 19193342 17632216 19997080 20680028 20504252 26880915 27217270 19434072 17016522 25032030

Sources:
TdgClinicalTrial ChemblInteractions TEND PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Serdolect

PMIDs:
11594443 16925508

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Serotonin 2c (5-HT2c) receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)