舒托必利在人和几种动物物种中的生物转化。

Biotransformation of sultopride in man and several animal species.

作者信息

Kobari T, Namekawa H, Kato Y, Yamada S

出版信息

Xenobiotica. 1985 Jun;15(6):469-76. doi: 10.3109/00498258509045020.

Abstract

The biotransformation of sultopride has been investigated in rat, rabbit, dog and man. In man sultopride was metabolically stable, and about 90% of an oral dose was excreted in urine unchanged and 4% as oxo-sultopride. Rat, rabbit and dog metabolized sultopride more extensively and excreted less than 40% of an oral dose of 14C-sultopride in urine. Four similar metabolites were excreted by the three animal species but the relative portions differed. The major radioactive component in rat urine was O-desmethyl sultopride, whereas oxo-sultopride and O-desmethyl sultopride were the major urinary metabolites in rabbit. Dog formed N-desethyl sultopride and oxo-sultopride as major urinary metabolites. The male rat excreted smaller amounts of unchanged sultopride in urine than did the female rat. The unchanged sultopride excreted in rat urine was increased slightly by repeated administration.

摘要

已在大鼠、兔子、狗和人体中研究了舒托必利的生物转化。在人体中，舒托必利代谢稳定，口服剂量的约90%以原形经尿液排出，4%以氧代舒托必利形式排出。大鼠、兔子和狗对舒托必利的代谢更广泛，口服剂量的14C-舒托必利经尿液排出的量不到40%。这三种动物物种排泄出四种相似的代谢物，但相对比例不同。大鼠尿液中的主要放射性成分是O-去甲基舒托必利，而氧代舒托必利和O-去甲基舒托必利是兔子尿液中的主要代谢物。狗形成N-去乙基舒托必利和氧代舒托必利作为主要尿液代谢物。雄性大鼠经尿液排泄的原形舒托必利量比雌性大鼠少。重复给药后，大鼠尿液中排泄的原形舒托必利略有增加。