5-HT2C agonist
5-HT2C serotonin receptor agonist
- Enhances serotonin’s appetite-suppressing brake → weight loss
- ↑ prolactin
- Decreased locomotor activity in animal models
Drugs with this mechanism (4)
- Fenfluramine — Serotonin releaser once in "fen-phen"; now for Dravet seizures, valvulopathy risk.
- Lorcaserin — 5-HT2C agonist weight-loss drug withdrawn for a cancer signal.
- mCPP — Trazodone and nefazodone metabolite; 5-HT2C agonist causing anxiety and dysphoria; accumulates when CYP2D6 is inhibited.
- Serotonin — The endogenous ligand at fourteen receptor subtypes; the home of serotonicity — synaptic serotonin elevation.
Self-check
- How does 5-HT2C agonism affect appetite and weight?
Suppresses appetite, promoting weight loss. - In what setting has reduced locomotor activity been observed with 5-HT2C agonism?
Animal models.
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