Synthesis and biological activities of metabolites of mosapride, a new gastroprokinetic agent

Chem Pharm Bull (Tokyo). 1995 Apr;43(4):699-702. doi: 10.1248/cpb.43.699.

Abstract

In order to confirm the proposed structures of two metabolites 3 and 4 of the gastroprokinetic agent mosapride [4-amino-5-chloro-2-ethoxy-N-([4-(4-fluorobenzyl)-2-morpholinyl] methyl)benzamide, 2], the compounds were synthesized and their biological activity was examined. The structures of the metabolites were confirmed by means of comparison with the synthetic compounds. The serotonin 5-HT4 receptor agonistic activities of the metabolites were found to be less than that of mosapride.

MeSH terms

  • Animals
  • Benzamides / chemical synthesis*
  • Benzamides / chemistry
  • Benzamides / pharmacology
  • Gastrointestinal Agents / chemical synthesis*
  • Gastrointestinal Agents / chemistry
  • Gastrointestinal Agents / pharmacology
  • Guinea Pigs
  • Ileum / drug effects
  • Ileum / physiology
  • In Vitro Techniques
  • Male
  • Morpholines / chemical synthesis*
  • Morpholines / chemistry
  • Morpholines / pharmacology
  • Serotonin Receptor Agonists / pharmacology

Substances

  • Benzamides
  • Gastrointestinal Agents
  • Morpholines
  • Serotonin Receptor Agonists
  • mosapride