非那吡啶在Fischer-344大鼠和B6C3F1小鼠肝细胞中的代谢。

Metabolism of methapyrilene by Fischer-344 rat and B6C3F1 mouse hepatocytes.

Kelly D W, Holder C L, Korfmacher W A, Getek T A, Lay J O, Casciano D A, Shaddock J G, Duhart H M, Slikker W

National Center for Toxicological Research, Jefferson, Arkansas 72079-9502.

Xenobiotica. 1992 Dec;22(12):1367-81. doi: 10.3109/00498259209056688.

Abstract

Suspension cultures of freshly isolated F344 rat and B6C3F1 mouse hepatocytes were compared for their ability to transform various concentrations of methapyrilene (MP). 2. MP metabolites were isolated and purified by h.p.l.c., and were identified by comparing their chromatographic and mass spectral properties with those of authentic standards. 3. Both rat and mouse hepatocytes transformed MP to tentatively identified 2-thiophenecarboxylic acid (I), and definitively identified mono-N-desmethyl methapyrilene glucuronide (II), methapyrilene glucuronide (III), methapyrilene N-oxide (V), and mono-N-desmethyl methapyrilene (VII).

摘要

比较了新鲜分离的F344大鼠和B6C3F1小鼠肝细胞的悬浮培养物对不同浓度美吡拉敏（MP）的转化能力。2. 通过高效液相色谱法分离和纯化MP代谢物，并通过将其色谱和质谱特性与标准品的特性进行比较来鉴定。3. 大鼠和小鼠肝细胞均将MP转化为初步鉴定的2-噻吩羧酸（I），并明确鉴定出单-N-去甲基美吡拉敏葡糖醛酸苷（II）、美吡拉敏葡糖醛酸苷（III）、美吡拉敏N-氧化物（V）和单-N-去甲基美吡拉敏（VII）。