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Target intelligence / Profile preview
Serotonin 5-hydroxytryptamine receptor 3 (5-HT3)
- Target
- 5-HT3
- Molecular classification
- Ligand-gated ion channel, Cys-loop superfamily, Receptor
01
Overview
The serotonin 5-hydroxytryptamine receptor 3 (5-HT3) is a ligand-gated ion channel that mediates fast excitatory neurotransmission in both the central and peripheral nervous systems by allowing cation influx upon activation by serotonin (5-HT). It is a pentameric complex, with both homopentameric (5-HT3A subunits only) and heteropentameric (e.g., 5-HT3A with 5-HT3B) forms. Activation leads to Na⁺ and K⁺ influx, causing neuronal depolarization/excitation and triggering neurotransmitter release. Clinically important antagonists like ondansetron and granisetron are used as antiemetics.
- Other names
- 5-HT3 receptor5-hydroxytryptamine receptor 3HTR3
02
Mechanism of action
Blocks vagal afferent signaling from gut enterochromaffin cells via inhibition of this receptor subtype.
03
Biological functions
Neuronal excitationNeurotransmitter releaseEmesis regulationPain perception modulationAnxiety modulationGastrointestinal motility regulationDrug reward pathway regulationNeuronal depolarization
04
Disease associations
EmesisNauseaVomitingPsychiatric disordersSubstance abuseAnxiety
05
Interacting drugs
Ondansetron
1 more in the full profile.
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