Mosapride citrate

Описание

Mosapride is an agonist of the serotonin (5-HT) receptor subtype 5-HT₄ (K_i = 69.9 nM). It is selective for 5-HT₄ over 5-HT₁, 5-HT₂, dopamine D₂, and α₁- and α₂-adrenergic receptors but acts as a partial antagonist at 5-HT₃ (K_i = 1,189 nM). It induces relaxation of precontracted rat esophageal thoracic muscularis mucosa preparations and enhances electrically evoked contractions in isolated guinea pig ileum (EC₅₀s = 208.4 and 73.2 nM, respectively). Mosapride (0.5 and 1 mg/kg, i.v.) increases antral and duodenal, but not ileal or colonic, motility in conscious dogs. It also increases gastric emptying in rats when administered at doses ranging from 0.03 to 30 mg/kg.

Использование

As a selective SR-4 activator and a SR-3 inhibitor, Mosapride(Mosapride citrate) is a gastroprokinetic agent that acts as a selective 5HT4 agonist which accelerates gastric emptying and is used for the treatment of acid reflux, irritable bowel syndrome and functional dyspepsia.

Биологическая активность

5-HT 4 receptor agonist and 5-HT 3 receptor antagonist. Displays no activity at D 2 , α 1 , α 2 , 5-HT 1 and 5-HT 2 receptors. Gastroprokinetic agent; increases gastric emptying in rats and stimulates gastric motor actvity in conscious dogs.