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大鼠体内丙环定的体外代谢

In vitro metabolism of procyclidine in the rat.

作者信息

Paeme G, Grimee R, Vercruysse A

出版信息

Eur J Drug Metab Pharmacokinet. 1984 Oct-Dec;9(4):311-3. doi: 10.1007/BF03189682.

Abstract

Procyclidine, 1-cyclohexyl-1-phenyl-3-(1-pyrrolidinyl)-1-propanol, was incubated with the 9000g supernatant fraction of rat liver homogenates, fortified with a NADPH generating system. Three major metabolites were isolated from the incubation mixture. They were identified as 1-(cis-4-hydroxycyclohexyl)-1-phenyl-3-(1-pyrrolidinyl)-1-propanol, 1-(trans-4-hydroxycyclohexyl)-1-phenyl-3-(1-pyrrolidinyl)-1-propanol, and (1R*, 3R*, 7S(R?)*)-1-(trans-3-hydroxycyclohexyl)-1-phenyl-3-(1-pyrrolidinyl) -1-propanol. The latter has not been detected previously in rat urine and probably represents an intermediate metabolite.

摘要

丙环定,即1-环己基-1-苯基-3-(1-吡咯烷基)-1-丙醇,与添加了NADPH生成系统的大鼠肝脏匀浆9000g上清液部分一起孵育。从孵育混合物中分离出三种主要代谢物。它们被鉴定为1-(顺式-4-羟基环己基)-1-苯基-3-(1-吡咯烷基)-1-丙醇、1-(反式-4-羟基环己基)-1-苯基-3-(1-吡咯烷基)-1-丙醇和(1R*, 3R*, 7S(R?)*)-1-(反式-3-羟基环己基)-1-苯基-3-(1-吡咯烷基)-1-丙醇。后者以前在大鼠尿液中未被检测到,可能代表一种中间代谢物。

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