Mosapride is an agonist of the serotonin (5-HT) receptor subtype 5-HT
4 (K
i = 69.9 nM).
1,2 It is selective for 5-HT
4 over 5-HT
1, 5-HT
2, dopamine D
2, and α
1- and α
2-adrenergic receptors but acts as a partial antagonist at 5-HT
3 (K
i = 1,189 nM).
1,2 It induces relaxation of precontracted rat esophageal thoracic muscularis mucosa preparations and enhances electrically evoked contractions in isolated guinea pig ileum (EC
50s = 208.4 and 73.2 nM, respectively).
3 Mosapride (0.5 and 1 mg/kg, i.v.) increases antral and duodenal, but not ileal or colonic, motility in conscious dogs.
1 It also increases gastric emptying in rats when administered at doses ranging from 0.03 to 30 mg/kg.
