Mosapride

Description

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.

Chemical properties

White to Off-White Crystalline Solid

Originator

Dainippon (Japan)

The Uses of Mosapride

gastroprokinetic agent

The Uses of Mosapride

A selective 5-HT4 receptor agonist. Gastroprokinetic.

What are the applications of Application

Mosapride is a gastroprokinetic, selective SR-4 (5-HT4 receptor) agonist

Definition

ChEBI: Mosapride is a racemate comprising equimolar amounts of (R)- and (S)-mosapride. It is a gastroprokinetic agent which acts on 5-hydroxytryptamine type 4 (5-HT4) receptors in the gastrointestinal plexus, consequently increasing the release of acetylcholine and hence enhancing gastrointestinal motility and gastric emptying. It has a role as a gastrointestinal drug and a serotonergic agonist. It contains a (R)-mosapride and a (S)-mosapride.

brand name

Gasmotin

Hazard

A poison by ingestion.

Safety Profile

A poison by ingestion. When heated to decomposition it emits toxic vapors of NOx, F-, and Cl-.