丙氧芬在大鼠肝脏中的体外代谢：一种甲醇代谢物与乙醛的反应。

In vitro metabolism of propoxyphene in rat liver: reaction of a carbinol metabolite with acetaldehyde.

作者信息

Hermansson I, Hermansson J, Stjernström N E

出版信息

Acta Pharmacol Toxicol (Copenh). 1983 Oct;53(4):257-64. doi: 10.1111/j.1600-0773.1983.tb03421.x.

DOI:10.1111/j.1600-0773.1983.tb03421.x

Abstract

The metabolism of the analgesic drug propoxyphene (alpha-d-propoxyphene) has been investigated in the rat liver 9,000 X g supernatant fraction. The incubations were analyzed by HPLC. The major metabolite was norpropoxyphene carbinol, obtained through demethylation and ester hydrolysis. The demethylated metabolite of propoxyphene, norpropoxyphene, was also detected. Addition of acetaldehyde to the incubation mixture decreased the metabolism of propoxyphene. Reactions between norpropoxyphene carbinol and acetaldehyde resulted in a fast disappearance of the carbinol and the formation of a reaction product, the significance of which is discussed.

摘要

已在大鼠肝脏9000×g上清液组分中研究了镇痛药丙氧芬（α-d-丙氧芬）的代谢。通过高效液相色谱法分析孵育物。主要代谢产物是去甲丙氧芬甲醇，它是通过去甲基化和酯水解得到的。还检测到了丙氧芬的去甲基化代谢产物去甲丙氧芬。向孵育混合物中添加乙醛会降低丙氧芬的代谢。去甲丙氧芬甲醇与乙醛之间的反应导致甲醇快速消失并形成一种反应产物，文中对其意义进行了讨论。