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曲吡那敏和苯吡胺在大鼠体内的N-去吡啶化和N-去二甲基氨基乙基化。新的代谢途径。

N-depyridination and N-dedimethylaminoethylation of tripelennamine and pyrilamine in the rat. New metabolic pathways.

作者信息

Yeh S Y

机构信息

National Institute on Drug Abuse, Addiction Research Center, Baltimore, MD 21224.

出版信息

Drug Metab Dispos. 1990 Jul-Aug;18(4):453-61.

PMID:1976067
Abstract

N-(2-Dimethylaminoethyl)benzylamine and 2-benzylaminopyridine were identified as two new urinary metabolites of tripelennamine in the rat by GC/MS. 2-(4-Methoxybenzylamino)-pyridine and N-(dimethylaminoethyl)-4-hydroxybenzylamine were identified as new urinary metabolites of pyrilamine by GC/MS. Thus, in addition to N- and O-demethylation, hydroxylation, and glucuronidation, N-debenzylation, N-depyridination and N-dedimethylaminoethylation were shown to be novel pathways for metabolism of tripelennamine and pyrilamine. The mechanism for N-depyridination and N-dealkylation is discussed.

摘要

通过气相色谱/质谱法(GC/MS),N-(2-二甲基氨基乙基)苄胺和2-苄氨基吡啶被鉴定为大鼠体内曲吡那敏的两种新的尿液代谢物。通过GC/MS,2-(4-甲氧基苄氨基)吡啶和N-(二甲基氨基乙基)-4-羟基苄胺被鉴定为吡苄明的新的尿液代谢物。因此,除了N-去甲基化、O-去甲基化、羟基化和葡萄糖醛酸化外,N-去苄基化、N-去吡啶基化和N-去二甲基氨基乙基化被证明是曲吡那敏和吡苄明代谢的新途径。本文讨论了N-去吡啶基化和N-脱烷基化的机制。

相似文献

1
N-depyridination and N-dedimethylaminoethylation of tripelennamine and pyrilamine in the rat. New metabolic pathways.曲吡那敏和苯吡胺在大鼠体内的N-去吡啶化和N-去二甲基氨基乙基化。新的代谢途径。
Drug Metab Dispos. 1990 Jul-Aug;18(4):453-61.
2
N-debenzylation of pyrilamine and tripelennamine in the rat. A new metabolic pathway.大鼠体内吡苄明和曲吡那敏的N-去苄基化作用。一条新的代谢途径。
Drug Metab Dispos. 1987 Jul-Aug;15(4):466-72.
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Quantitative metabolic profile of tripelennamine and pyrilamine in the rat.曲吡那敏和吡苄明在大鼠体内的定量代谢概况
Drug Metab Dispos. 1988 May-Jun;16(3):499-502.
4
The metabolism and elimination of pyrilamine maleate in the rat.马来酸氯苯那敏在大鼠体内的代谢与消除。
Drug Metab Dispos. 1987 Jul-Aug;15(4):460-5.
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Microbial transformation of the antihistamine pyrilamine maleate. Formation of potential mammalian metabolites.
Drug Metab Dispos. 1987 Jan-Feb;15(1):97-106.
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A comparative in vitro metabolic study of methaphenilene and pyribenzamine.美沙芬林与吡苄明的体外代谢对比研究。
Xenobiotica. 1988 Sep;18(9):1085-96. doi: 10.3109/00498258809042231.
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Characterization of doxylamine and pyrilamine metabolites via thermospray/mass spectrometry and tandem mass spectrometry.通过热喷雾/质谱和串联质谱对多西拉敏和吡苄明代谢物进行表征。
Biomed Environ Mass Spectrom. 1988 May 1;15(9):501-8. doi: 10.1002/bms.1200150907.
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Fungal transformations of antihistamines: metabolism of methapyrilene, thenyldiamine and tripelennamine to N-oxide and N-demethylated derivatives.
Xenobiotica. 1988 Mar;18(3):301-12. doi: 10.3109/00498258809041666.
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Metabolism of tripelennamine in man.
Drug Metab Dispos. 1976 Jul-Aug;4(4):372-8.
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Metabolism, tissue distribution and covalent binding of tripelennamine and its N-nitroso derivative in the rat.曲吡那敏及其N-亚硝基衍生物在大鼠体内的代谢、组织分布和共价结合
J Pharmacol Exp Ther. 1975 Dec;195(3):433-40.

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