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Serotonin receptor type 2C (5-HT2C receptor)

Target
5-HT2C receptor
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

The serotonin receptor type 2C (5-hydroxytryptamine receptor 2C, abbreviated as 5‑HT₂C) is a member of the G protein-coupled receptor family that binds the endogenous neurotransmitter serotonin. It mediates excitatory neurotransmission via coupling to Gq/11 proteins. The human gene encoding this protein is HTR2C, located on the X chromosome. This receptor plays important roles in regulating mood, appetite control, endocrine secretion, motor function modulation, and cerebrospinal fluid volume regulation. It has been implicated in several neuropsychiatric disorders—including depression and anxiety—as well as obesity. Drugs targeting this site include both selective agonists and antagonists developed for research into CNS diseases and potential therapies for obesity. Polymorphisms within its gene can affect disease risk differently between sexes due to its X-linked inheritance pattern.

Other names
5-hydroxytryptamine receptor 2CHTR2CSerotonin 2c receptor5-HT₂C5-HT1C
02

Mechanism of action

Drugs targeting this molecule act primarily by modulating serotonin signaling through the following mechanisms: - Agonism at the GPCR to stimulate downstream signaling via Gq/11 proteins, increasing IP3/DAG pathway activity and excitatory neurotransmission. - Antagonism or inverse agonism to block or reduce serotonin-mediated effects at this site.

03

Biological functions

Signal transductionExcitatory neurotransmissionRegulation of cerebrospinal fluid volume
04

Disease associations

Neuropsychiatric disorders, including depression, obsessive-compulsive disorder, and anxiety-related conditionsObesity and metabolic disorders
05

Safety considerations

Risk of psychiatric side effects such as anxiety, agitation, hallucinations with some agonists.Potential metabolic disturbances including weight gain or loss depending on drug action.Sex-specific differences due to X-linked gene location affecting expression/polymorphism impact.
06

Interacting drugs

mCPP (meta-chlorophenylpiperazine)

7 more in the full profile.

07

Biomarkers

No widely established clinical biomarkers specific for patient selection or efficacy monitoring of drugs targeting only the serotonin receptor type 2C.Genetic polymorphisms in HTR2C may influence drug response or disease susceptibility in psychiatric and metabolic conditions.

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