5-HT4 agonist
5-HT4 serotonin receptor agonist
- Enhances enteric acetylcholine release → ↑ GI motility and transit
- Prokinetic: treats constipation and gastroparesis-spectrum symptoms
- Possible pro-cognitive effect (early human studies)
Drugs with this mechanism (3)
- Cisapride — 5-HT4 prokinetic withdrawn for fatal QT arrhythmias.
- Prucalopride — Selective 5-HT4 agonist prokinetic for chronic constipation.
- Serotonin — The endogenous ligand at fourteen receptor subtypes; the home of serotonicity — synaptic serotonin elevation.
Self-check
- Which enteric transmitter does 5-HT4 agonism increase?
Acetylcholine. - How established is the proposed cognitive benefit of 5-HT4 agonism?
Possible benefit in early human studies.
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