4-アミノ-5-クロロ-2-エトキシ-N-[[4-(4-フルオロベンジル)モルホリン-2-イル]メチル]ベンズアミド·シトラート

プロパティ

安全情報

説明

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.