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大鼠肝微粒体对4-(3-环己基丙酰基)-1-(2-乙氧基苯基)哌嗪(D-16120)的代谢

Metabolism of 4-(3-cyclohexylpropionyl)-1-(2-ethoxyphenyl) piperazine (D-16120) by rat liver microsomes.

作者信息

Caputo O, Rocco F, Grosa G

机构信息

Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, Italy.

出版信息

Eur J Drug Metab Pharmacokinet. 1994 Oct-Dec;19(4):303-10. doi: 10.1007/BF03188856.

Abstract

The metabolic fate of central analgesic 4-(3-cyclohexylpropionyl)-1-(2-ethoxyphenyl) piperazine (D-16120), was studied in vitro with phenobarbital 3-methylcholanthrene and clofibrate induced rat liver microsomal fractions. The presence of four metabolites was directly or indirectly established. Biotransformation products were isolated by TLC and HPLC techniques and, when possible, the structures were confirmed through comparison with synthetic samples. The metabolic pathways involved are oxidative dealkylation, aromatic and alicyclic hydroxylation.

摘要

利用苯巴比妥、3-甲基胆蒽和氯贝丁酯诱导的大鼠肝微粒体组分,在体外研究了中枢镇痛药4-(3-环己基丙酰基)-1-(2-乙氧基苯基)哌嗪(D-16120)的代谢命运。直接或间接确定了四种代谢产物的存在。通过薄层色谱法(TLC)和高效液相色谱法(HPLC)技术分离生物转化产物,并在可能的情况下,通过与合成样品比较来确认其结构。所涉及的代谢途径包括氧化脱烷基、芳环和脂环羟基化。

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