Target intelligence / Profile preview

Serotonin Receptor 5-HT₂C (5-HT2C)

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

Overview

The 5-HT₂C receptor is a subtype of serotonin receptor, part of the 5-HT2 family, and a G protein-coupled receptor (GPCR) primarily coupled to the Gq/G11 protein. It mediates excitatory neurotransmission and is widely distributed in the central nervous system and, to a lesser extent, in peripheral tissues. It plays significant roles in regulating mood, anxiety, feeding behavior, and reproductive behavior. Drugs targeting the 5-HT₂C receptor are used or investigated for obesity, schizophrenia, drug abuse, and migraine. Agonists include endogenous serotonin and ergotamine; ritanserin acts as an inverse agonist. Ligand binding induces characteristic shifts in transmembrane helices that underlie activation or inhibition of signaling pathways.

Other names
5-Hydroxytryptamine Receptor 2CHTR2C
02

Mechanism of action

Agonist or antagonist binding to the 5-HT2C receptor modulates downstream signaling pathways via Gq/G11 protein coupling, influencing neurotransmitter release and neuronal excitability.

03

Biological functions

NeurotransmissionMood regulationAnxiety regulationFeeding behavior regulationReproductive behavior regulationDopamine modulationHormone secretion regulation
04

Disease associations

ObesitySchizophreniaDrug abuseMigraineMood disorders
05

Safety considerations

Selectivity challenges due to similarity with other serotonin receptors.Potential for off-target effects.
06

Interacting drugs

Serotonin

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