{"title":"In vitro metabolism of propoxyphene in rat liver: reaction of a carbinol metabolite with acetaldehyde.","authors":"I Hermansson, J Hermansson, N E Stjernström","doi":"10.1111/j.1600-0773.1983.tb03421.x","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":6972,"journal":{"name":"Acta pharmacologica et toxicologica","volume":"53 4","pages":"257-64"},"PeriodicalIF":0.0000,"publicationDate":"1983-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1600-0773.1983.tb03421.x","citationCount":"4","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Acta pharmacologica et toxicologica","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1111/j.1600-0773.1983.tb03421.x","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 4
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.
研究了镇痛药丙氧芬(α -d-丙氧芬)在大鼠肝脏9000 X g上清液中的代谢。用高效液相色谱法对培养物进行分析。主要代谢产物为去甲基化和酯水解得到的去丙氧苯甲醇。丙氧基的去甲基代谢物去甲丙氧基也被检测到。在培养液中加入乙醛会降低丙氧苯的代谢。降丙氧苯甲醇与乙醛反应后，甲醇迅速消失并生成反应产物，讨论了其意义。
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