Mosapride citrate, a new gastroprokinetic benzamide was introduced in
Japan as Gasmotin for the relief of gastrointestinal symptoms in patients with
chronic gastritis, gastro-oesophageal reflux, dyspepsia and post-surgery use.
Mosapride is synthesized by final amidation between the corresponding benzoic
acid, itself obtained in 3 steps from methyl 4-acetamido salicylate, and the
appropriate 2-aminomethyl-morpholine. Mosapride is a 5-HT4 partial agonist
without notable activity for D2, 5-HT1 , 5-HT2, alpha-1 and alpha-2 receptors. In
dogs, mosapride was as potent as cisapride to stimulate antral and duodenal
motility. In most of species including man, mosapride undergoes extensive
cleavage to a N-debenzylated metabolite which retains partial 5-HT4 activity but
has potent 5-HT3 antagonist activity.
