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γ-咔啉类抗心律失常及心脏保护剂司托巴定在大鼠肝微粒体中的生物转化

Biotransformation of stobadine, a gamma-carboline antiarrhythmic and cardioprotective agent, in rat liver microsomes.

作者信息

Stefek M, Benes L, Jergelová M, Scasnár V, Turi-Nagy L, Kocis P

机构信息

Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, Czechoslovakia.

出版信息

Xenobiotica. 1987 Sep;17(9):1067-73. doi: 10.3109/00498258709044205.

DOI:10.3109/00498258709044205
PMID:3687063
Abstract
  1. The metabolism of stobadine, a gamma-carboline antiarrhythmic and cardioprotective agent, was investigated in vitro using fortified rat liver microsomal preparations. 2. Two metabolic products, N-desmethyl stobadine and stobadine N-oxide were isolated and identified by means of t.l.c.,g.l.c. -mass spectrometry, n.m.r. spectrometry and comparison with synthetic reference compounds. 3. Stobadine N-oxide was resolved into two optically active stereoisomers which were produced enzymically in approximately equal quantities.
摘要
  1. 使用强化大鼠肝微粒体制剂在体外研究了γ-咔啉类抗心律失常和心脏保护剂司托巴定的代谢。2. 通过薄层层析、气相色谱-质谱联用、核磁共振光谱以及与合成参考化合物比较,分离并鉴定了两种代谢产物,N-去甲基司托巴定和司托巴定N-氧化物。3. 司托巴定N-氧化物被拆分为两种光学活性立体异构体,它们是通过酶促反应以大致相等的量产生的。

相似文献

1
Biotransformation of stobadine, a gamma-carboline antiarrhythmic and cardioprotective agent, in rat liver microsomes.γ-咔啉类抗心律失常及心脏保护剂司托巴定在大鼠肝微粒体中的生物转化
Xenobiotica. 1987 Sep;17(9):1067-73. doi: 10.3109/00498258709044205.
2
Hydrogen peroxide-dependent liver microsomal N-demethylation and N-oxygenation of stobadine, a gamma-carboline antiarrhythmic and cardioprotective agent.过氧化氢依赖性肝微粒体对斯托巴定的N-去甲基化和N-氧化作用,斯托巴定是一种γ-咔啉类抗心律失常和心脏保护剂。
Xenobiotica. 1989 Jun;19(6):627-34. doi: 10.3109/00498258909042299.
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Gas chromatographic determination of stobadine, N-desmethylstobadine and stobadine N-oxide in rat liver microsomal incubations.气相色谱法测定大鼠肝微粒体孵育液中的司巴丁、N-去甲基司巴丁和司巴丁N-氧化物。
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引用本文的文献

1
Overview of stobadine bioanalysis: evaluation and application in pharmacokinetics.司托巴定生物分析概述:在药代动力学中的评估与应用
Eur J Drug Metab Pharmacokinet. 1999 Jul-Sep;24(3):237-42. doi: 10.1007/BF03190026.
2
The pyridoindole antioxidant stobadine inhibited glycation-induced absorbance and fluorescence changes in albumin.
Acta Diabetol. 1996 Mar;33(1):35-40. doi: 10.1007/BF00571938.