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

RenMab: F1 (+/-)

Drug Information

Launched drugs: 26
Drugs in clinical trials: 22
Latest Research Phase: Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Lumateperone

ITI-007, ITI-722

Approved

Bristol-Myers Squibb Company

Schizophrenia, Depressive Disorder, Major, Bipolar Disorder, Alzheimer Disease

Aripiprazole Lauroxil

RDC-3317, ALKS-9070, ALKS-9072

Approved

Alkermes Plc

Schizophrenia, Psychotic Disorders, Bipolar Disorder

Blonanserin

AD-5423, DSP-5423, DSP-5423P

Approved

Sumitomo Dainippon Pharma Co Ltd

Schizophrenia

Pimavanserin Tartrate

ACP-103, BVF-048

Approved

Acadia Pharmaceuticals

Schizophrenia, Depressive Disorder, Major, Psychotic Disorders, Hallucinations, Parkinson Disease, Delusions, Alzheimer Disease, Neurodegenerative Diseases

Asenapine Maleate

HP-3070, ME-2136, MK-8274, Org-5222, SCH-900274

Approved

Merck Sharp & Dohme Corp

Schizophrenia, Psychotic Disorders, Bipolar Disorder, Schizophrenia, Paranoid, Schizophrenia, Disorganized

Perospirone Hydrochloride Hydrate

SM-9018

Approved

Sumitomo Dainippon

Schizophrenia, Bipolar Disorder

Olanzapine/Samidorphan

ALKS-3831

Approved

Alkermes Plc

Schizophrenia, Psychotic Disorders, Bipolar Disorder, Alcoholism

Olanzapine

ALKS-7921, LY-170052, LY-170053

Approved

Eli Lilly And Company

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

Sertindole

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

Approved

Schizophrenia, Cognition

Clozapine

LEX-123

Approved

Hls Therapeutics Inc

Schizophrenia

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)