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


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





Clinical Trials


ITI-007, ITI-722


Bristol-Myers Squibb Company

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

Aripiprazole Lauroxil

RDC-3317, ALKS-9070, ALKS-9072


Alkermes Plc

Schizophrenia, Psychotic Disorders, Bipolar Disorder


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


Sumitomo Dainippon Pharma Co Ltd


Pimavanserin Tartrate

ACP-103, BVF-048


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


Merck Sharp & Dohme Corp

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

Perospirone Hydrochloride Hydrate



Sumitomo Dainippon

Schizophrenia, Bipolar Disorder




Alkermes Plc

Schizophrenia, Psychotic Disorders, Bipolar Disorder, Alcoholism


ALKS-7921, LY-170052, LY-170053


Eli Lilly And Company

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


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


Schizophrenia, Cognition




Hls Therapeutics Inc






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

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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

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

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

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

The DNA sequence and analysis of human chromosome 13

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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)