Mosapride (citrate)

Mosapride is an agonist of the serotonin (5-HT) receptor subtype 5-HT₄ (K_i = 69.9 nM).^1,2 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).^1,2 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).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.

WARNING This product is not for human or veterinary use.

1. Yoshida, N., Omoya, H., Oka, M., et al. AS-4370, a novel gastrokinetic agent free of dopamine D₂ receptor antagonist properties. Arch. Int. Pharmacodyn. Ther. 300, 51-67 (1989).

2. Hirokawa, Y., Fujiwara, I., Suzuki, K., et al. Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT₃ and dopamine D₂ receptor antagonistic activity. J. Med. Chem. 46(5), 702-715 (2003).

3. Mine, Y., Yoshikawa, T., Oku, S., et al. Comparison of effect of mosapride citrate and existing 5-HT₄ receptor agonists on gastrointestinal motility in vivo and in vitro. J. Pharmacol. Exp. Ther. 283(3), 1000-1008 (1997).