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抗帕金森病药物布地品在大鼠体内的代谢转归。

The metabolic fate of the anti-parkinsonian drug budipine in rats.

作者信息

Caputo O, Grosa G, Ceruti M, Rocco F, Biglino G

机构信息

Istituto di Chimica Farmaceutica Applicata, Università di Torino, Italy.

出版信息

Eur J Drug Metab Pharmacokinet. 1991 Apr-Jun;16(2):113-8. doi: 10.1007/BF03189947.

Abstract

The metabolic fate of the anti-Parkinsonian drug budipine was studied in rats after oral administration. The presence of an aromatic hydroxylation product, metabolite M1, and its O-sulphate conjugate was confirmed. Three new minor metabolites, budipine N-oxide, metabolite M1 N-oxide and a secondary metabolite derived from M1 via hydroxylation of a methyl of the tert-butyl group, were isolated and identified in rat urine. The presence of a metabolite M1-glucuronic acid conjugate, was also established through different enzymatic treatments of the rat urine.

摘要

在大鼠口服给予抗帕金森病药物布地品后,对其代谢命运进行了研究。确认了一种芳香族羟基化产物、代谢物M1及其O - 硫酸酯共轭物的存在。在大鼠尿液中分离并鉴定出三种新的次要代谢物,即布地品N - 氧化物、代谢物M1 N - 氧化物以及一种通过叔丁基甲基羟基化从M1衍生而来的二级代谢物。通过对大鼠尿液进行不同的酶处理,还确定了代谢物M1 - 葡萄糖醛酸共轭物的存在。

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