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Serotonin Receptor Subtype 5-HT2C
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The 5-HT2C receptor is a subtype of the serotonin receptor family, acting as a G protein-coupled receptor primarily coupled to Gq/11 proteins. It is highly expressed in the central nervous system and plays critical roles in regulating food intake, anxiety, and other functions. Polymorphisms in the HTR2C gene are associated with psychiatric disorders, substance use disorders, obesity, and other conditions, making it a target for antipsychotics, appetite suppressants, and other potential therapeutic agents.
02
Mechanism of action
Agonism or antagonism of the 5-HT2C receptor, leading to downstream effects via Gq/11 signaling (PLCβ activation, IP₃/DAG production, Ca²⁺/PKC activation) and potentially Gq/13 signaling (PLA₂ activation, arachidonic acid release, cGMP production).
03
Biological functions
NeurotransmissionSignal transductionAppetite regulationMood modulationAnxiety modulationMotoneuron control
04
Disease associations
ObesityDepressionAnxietySubstance use disordersPrader-Willi syndromeMigraineSexual dysfunction
05
Safety considerations
Off-target activity at related receptors (e.g., 5-HT2A, 5-HT2B) leading to hallucinations or cardiac issuesAnxiety-like behaviors with antagonists
06
Interacting drugs
Antipsychotics
4 more in the full profile.
07
Biomarkers
Polymorphisms in HTR2C gene
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