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体外微粒体制剂对3-取代吡啶进行N-氧化所涉及的一些因素。

Some factors involved in the N-oxidation of 3-substituted pyridines by microsomal preparations in vitro.

作者信息

Gorrod J W, Damani L A

出版信息

Xenobiotica. 1979 Apr;9(4):209-18. doi: 10.3109/00498257909038723.

DOI:10.3109/00498257909038723
PMID:483857
Abstract
  1. Pyridine-N-oxides have been identified as metabolites in vitro of several 3-substituted pyridines. 2. Factors affecting the metabolism of these pyridines in vitro have been studied, and conditions which give the most metabolism have been established. 3. 'Pyridine-N-oxidase' activity resides mainly in the hepatic and pulmonary microsomal fractions. 4. A species difference was evident with 'pyridine-N-oxidase' activity decreasing in the order hamster, rabbit, mouse, guinea-pig and rat. 5. A sex difference in 'pyridine-N-oxidase' activity was also established in rats and mice. 6. The appropriate kinetic factors, Km and Vmax for the N-oxidation of pyridine, 3-methylpyridine and 3-chloropyridine are reported.
摘要
  1. 吡啶-N-氧化物已被鉴定为几种3-取代吡啶的体外代谢产物。2. 已研究了影响这些吡啶体外代谢的因素，并确定了代谢最为活跃的条件。3. “吡啶-N-氧化酶”活性主要存在于肝脏和肺微粒体部分。4. 明显存在种属差异，“吡啶-N-氧化酶”活性按仓鼠、兔、小鼠、豚鼠和大鼠的顺序递减。5. 在大鼠和小鼠中也确定了“吡啶-N-氧化酶”活性的性别差异。6. 报道了吡啶、3-甲基吡啶和3-氯吡啶N-氧化的合适动力学因子Km和Vmax。

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Eur J Drug Metab Pharmacokinet. 1980;5(1):53-7. doi: 10.1007/BF03189445.
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Eur J Drug Metab Pharmacokinet. 1987 Oct-Dec;12(4):253-8. doi: 10.1007/BF03189908.
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