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Target intelligence / Profile preview
Serotonin Receptor 5HT2C (5HT2C)
- Target
- 5HT2C
- Molecular classification
- GPCR, Receptor
01
Overview
The serotonin receptor 5HT2C (5-hydroxytryptamine receptor 2C or HTR2C) is a G protein-coupled receptor (GPCR) that binds serotonin. It is expressed in the choroid plexus, hippocampus, amygdala, substantia nigra, and other brain regions, and is involved in mood, appetite, anxiety, temperature regulation, locomotion, and sexual function. It signals through Gq/G11 proteins, activating PLC and increasing intracellular Ca2+. Therapeutic interest includes obesity, psychiatric disorders, and substance use disorders. The receptor exists as a homodimer. Polymorphisms can have sex-specific effects due to X-chromosome localization.
- Other names
- 5-hydroxytryptamine receptor 2CHTR2C
02
Mechanism of action
Gq/G11 protein activation leading to PLC activation, IP3 production, and intracellular Ca2+ release; PLA2 activation; RhoA/PLD pathway activation; ERK signaling activation; Inhibition of dopamine and norepinephrine release.
03
Biological functions
Signal transductionMood regulationAppetite regulationAnxiety regulationTemperature regulationLocomotion modulationSexual behavior regulation
04
Disease associations
ObesityPsychiatric disordersDepressionBipolar disorderSubstance use disordersSexual dysfunctionsUrinary incontinence
05
Safety considerations
Sex-specific effects due to X-chromosome localizationPotential for off-target effects with synthetic ligands
06
Interacting drugs
Serotonin
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