Yeh S Y
National Institute on Drug Abuse, Addiction Research Center, Baltimore, MD 21224.
Drug Metab Dispos. 1990 Jul-Aug;18(4):453-61.
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.
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。