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诺米芬辛(阿立凡、美利他)的代谢:从人尿中分离并鉴定诺米芬辛 - 14C 的结合物

Metabolism of nomifensine (Alival, Merital): isolation and identification of the conjugates of nomifensine-14C from human urine.

作者信息

Hornke I, Fehlhaber H W, Girg M, Jantz H

出版信息

Br J Clin Pharmacol. 1980 Mar;9(3):255-64. doi: 10.1111/j.1365-2125.1980.tb04835.x.

Abstract

1 It can be stated in regard to the metabolism of nomifensine that the metabolites and also the starting compound are present in alkaline urine almost completely in conjugated form. 2 The metabolites M I-M III represent about 30% of the radioactivity excreted with urine. Two-thirds are N-glucuronides and one-third O-glucuronides. 3 Nearly the entire remainder of the renally eliminated radioactivity in nomifensine which is present in conjugated form as N-glucuronide. 4 Thus over 90% of the metabolites formed in man and excreted via urine have been identified.

摘要
  1. 关于诺米芬辛的代谢可以指出,其代谢产物以及起始化合物在碱性尿液中几乎完全以结合形式存在。2. 代谢产物M I - M III约占随尿液排出的放射性的30%。其中三分之二是N - 葡萄糖醛酸苷,三分之一是O - 葡萄糖醛酸苷。3. 诺米芬辛经肾脏排泄的放射性物质几乎全部以N - 葡萄糖醛酸苷的结合形式存在。4. 因此,已鉴定出在人体中形成并经尿液排出的代谢产物超过90%。

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