5HT2AR

Synonyms

HTR2A, HTR2, 5-Hydroxytryptamine Receptor 2A, 5-Hydroxytryptamine (Serotonin) Receptor 2A, G Protein-Coupled, 5-Hydroxytryptamine (Serotonin) Receptor 2A, Serotonin 5-HT-2A Receptor, Serotonin Receptor 2A, 5-HT2 Receptor, 5-HT-2A, 5-HT2A, 5-HT-2, Receptor, Serotonin, 5-HT2A, 5HT2AR

Description

5HT2AR is a g-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction.Acts as a receptor for human JC polyomavirus/JCPyV.

KO Status

F0

Drug Information

Launched drugs: 24
Drugs in clinical trials: 21
Latest Research Phase: Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Aripiprazole Lauroxil

RDC-3317, ALKS-9070, ALKS-9072

Approved

Alkermes Plc

Schizophrenia, Psychotic Disorders, Bipolar Disorder

Cariprazine Hydrochloride

MP-214, RGH-188, RGH-188 HCl

Approved

Gedeon Richter

Schizophrenia, Depressive Disorder, Major, Autism Spectrum Disorder, Depression, Bipolar Disorder

Naftidrofuryl Oxalate

LS-121, EU-1806

Approved

Peripheral Vascular Diseases, Cerebrovascular Disorders

Zotepine

FR-1314

Approved

Schizophrenia

Olanzapine

ALKS-7921, LY-170052, LY-170053

Approved

Eli Lilly And Company

Schizophrenia, Depression, Psychotic Disorders, Bipolar Disorder, Emergence Delirium, Vomiting, Depressive Disorder, Treatment-Resistant, Nausea, Borderline Personality Disorder, Fasting

Pipamperone Hydrochloride

R-3345

Approved

Mental Disorders

Sertindole

S-1991, Lu-23-174 (maleate)

Approved

Schizophrenia, Cognition

Paliperidone palmitate

R-092670, JNS-010, LY-03010, RO-92670

Approved

Janssen Global Services Llc

Schizophrenia, Psychotic Disorders

Clozapine

LEX-123

Approved

Hls Therapeutics Inc

Schizophrenia

Flibanserin

BIMT-17, BIMT-17-BS

Approved

Sprout Pharmaceuticals

Depression, Sexual Dysfunctions, Psychological

References


Title

Authors

Source

Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes

Saltzman A.G., Morse B., Whitman M.M., Ivanshchenko Y., Jaye M., Felder S.,

Biochem. Biophys. Res. Commun. 181:1469-1478(1991)

The human 5-HT2 receptor is encoded by a multiple intron-exon gene

Chen K., Yang W., Grimsby J., Shih J.C.,

Brain Res. Mol. Brain Res. 14:20-26(1992)

Primary structure of the human platelet serotonin 5-HT2A receptor: identify with frontal cortex serotonin 5-HT2A receptor

Cook E.H. Jr., Fletcher K.E., Wainwright M., Marks N., Yan S.Y., Leventhal B.L.,

J. Neurochem. 63:465-469(1994)

Complete sequencing and characterization of 21,243 full-length human cDNAs

Ota T., Suzuki Y., Nishikawa T., Otsuki T., Sugiyama T., Irie R., Wakamatsu A., Hayashi K., Sato H., Nagai K., Kimura K., Makita H., Sekine M., Obayashi M., Nishi T., Shibahara T., Tanaka T., Ishii S., Sugano S.,

Nat. Genet. 36:40-45(2004)

The DNA sequence and analysis of human chromosome 13

Dunham A., Matthews L.H., Burton J., Ashurst J.L., Howe K.L., Ashcroft K.J., Beare D.M., Burford D.C., Hunt S.E., Griffiths-Jones S., Jones M.C., Keenan S.J., Oliver K., Scott C.E., Ainscough R., Almeida J.P., Ambrose K.D., Andrews D.T., Ross M.T.,

Nature 428:522-528(2004)

The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)

The MGC Project Team,

Genome Res. 14:2121-2127(2004)

Genomic organization, coding sequence and functional expression of human 5-HT2 and 5-HT1A receptor genes

Stam N.J., van Huizen F., van Alebeek C., Brands J., Dijkema R., Tonnaer J.A., Olijve W.,

Eur. J. Pharmacol. 227:153-162(1992)

Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1

Becamel C., Figge A., Poliak S., Dumuis A., Peles E., Bockaert J., Luebbert H., Ullmer C.,

J. Biol. Chem. 276:12974-12982(2001)

The serotonin 5-HT2A and 5-HT2C receptors interact with specific sets of PDZ proteins

Becamel C., Gavarini S., Chanrion B., Alonso G., Galeotti N., Dumuis A., Bockaert J., Marin P.,

J. Biol. Chem. 279:20257-20266(2004)

Serotonin receptors

Nichols D.E., Nichols C.D.,

Chem. Rev. 108:1614-1641(2008)