Kato S, Morie T, Yoshida N
Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1995 Apr;43(4):699-702. doi: 10.1248/cpb.43.699.
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.
为了确证促胃肠动力药莫沙必利[4-氨基-5-氯-2-乙氧基-N-([4-(4-氟苄基)-2-吗啉基]甲基)苯甲酰胺,2]的两种代谢产物3和4的推测结构,合成了这些化合物并检测了它们的生物活性。通过与合成化合物进行比较确证了代谢产物的结构。发现这些代谢产物的5-羟色胺5-HT4受体激动活性低于莫沙必利。