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Wistar大鼠体内季铵化合物的亚硝化作用

Nitrosation of quaternary ammonium compounds in vivo in the Wistar rat.

作者信息

Maduagwu E N

出版信息

Xenobiotica. 1985 Dec;15(12):1061-8. doi: 10.3109/00498258509049101.

DOI:10.3109/00498258509049101
PMID:4090526
Abstract

Animals dosed orally with nitrite (1.5 X 10(-3) mol/kg) and nonyl dimethylbenzylammonium bromide (2.9 X 10(-4) mol/kg) exhibit liver damage within two hours; cetyl trimethylammonium bromide plus nitrite was not significantly hepatotoxic. Both nonyl dimethylbenzyl ammonium bromide and cetyl trimethylammonium bromide were demethylated by rat-liver microsomal preparations; substrate concentrations of 1 mM or more were inhibitory. Bile from rats given i.p. doses of cetyl trimethylammonium bromide, nonyl dimethylbenzylammonium bromide or dodecyl dimethylbenzylammonium bromide contains only metabolites, no unchanged compounds were detected.

摘要

口服给予亚硝酸盐(1.5×10⁻³摩尔/千克)和溴化壬基二甲基苄基铵(2.9×10⁻⁴摩尔/千克)的动物在两小时内出现肝脏损伤;十六烷基三甲基溴化铵加亚硝酸盐没有明显的肝毒性。溴化壬基二甲基苄基铵和十六烷基三甲基溴化铵都被大鼠肝脏微粒体制剂去甲基化;1毫摩尔或更高的底物浓度具有抑制作用。经腹腔注射给予十六烷基三甲基溴化铵、溴化壬基二甲基苄基铵或溴化十二烷基二甲基苄基铵的大鼠胆汁中仅含有代谢物,未检测到未变化的化合物。

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