Target intelligence / Profile preview

Serotonin Receptor 5-HT2C (5-HT2C receptor)

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

Overview

The 5-HT2C receptor is a G protein-coupled receptor (GPCR) that primarily couples to the Gq/G11 protein and mediates excitatory neurotransmission. It plays significant roles in regulating mood, anxiety, feeding behavior, and reproductive behavior. It also modulates dopamine release across several brain regions. Genetic variations are associated with susceptibility to psychiatric disorders, substance use disorders, and obesity. Drugs targeting the 5-HT2C receptor are used or investigated for treating obesity, drug abuse, and schizophrenia. Antagonists can stimulate dopaminergic pathways, potentially useful for counteracting SSRI-induced side effects or treating Parkinson’s disease. The receptor interacts with proteins such as MPDZ, which may influence its signaling properties.

Other names
5-hydroxytryptamine receptor 2CHTR2C
02

Mechanism of action

Agonism, antagonism, inverse agonism, allosteric modulation, depending on the drug and region of the brain.

03

Biological functions

NeurotransmissionMood regulationAppetite controlFeeding behaviorReproductive behaviorDopamine modulation
04

Disease associations

DepressionAnxiety disordersObsessive-compulsive disorderSubstance use disorderObesitySchizophreniaParkinson's diseasePrader–Willi syndrome
05

Safety considerations

SSRI-induced side effectsParadoxical behavioral outcomes depending on regional selectivity
06

Interacting drugs

Ergotamine

2 more in the full profile.

07

Biomarkers

HTR2C polymorphisms (associated with susceptibility to psychiatric disorders, substance use disorders, obesity)

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