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Target intelligence / Profile preview
Serotonin 2C Receptor (5-HT2C)
- Target
- 5-HT2C
- Molecular classification
- G protein-coupled receptor (GPCR), Receptor
01
Overview
The serotonin 2C receptor (5-HT2C) is a G protein-coupled receptor (GPCR) primarily expressed within the central nervous system. Upon activation by serotonin, it couples to Gq proteins, activating PLC, IP3, and Ca2+ signaling. It plays a critical role in regulating appetite, mood, locomotion, and endocrine function. Due to its involvement in key CNS processes, it represents a therapeutic target for obesity, psychiatric disorders, and substance use disorders. Drug development is complicated by cross-reactivity with other 5-HT2 receptor subtypes.
- Other names
- 5-Hydroxytryptamine Receptor 2CHTR2C
02
Mechanism of action
Agonist binding leads to activation of Gq proteins, phospholipase C (PLC), IP3 production, and intracellular Ca2+ release. Also activates phospholipase A2 (PLA2), RhoA/PLD pathway, and extracellular signal-regulated kinase (ERK) pathway.
03
Biological functions
Signal transductionRegulation of appetiteMood regulationRegulation of locomotionEndocrine modulationRegulation of synaptic transmission
04
Disease associations
ObesityPsychiatric disordersSubstance use disordersAnxiety
05
Safety considerations
Cross-reactivity with related 5-HT2 receptor subtypes complicating drug development.
06
Interacting drugs
Serotonin
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