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14C-环己胺在小鼠和两种品系大鼠体内的代谢

The metabolism of 14C-cyclohexylamine in mice and two strains of rat.

作者信息

Roberts A, Renwick A G

出版信息

Xenobiotica. 1985 Jun;15(6):477-83. doi: 10.3109/00498258509045021.

DOI:10.3109/00498258509045021
PMID:4036172
Abstract

After administration of 14C-cyclohexylamine (35-500 mg/kg) to male mice and rats, 80% of the dose of 14C was excreted in the urine, mostly within the first 24 h after dosing. In Wistar rats, 7-9% of the 14C in the 0-24 h urine was present as cis-4-aminocyclohexanol, with a similar amount as the corresponding 3-isomers. In the DA rat, only 1-2% of the 14C, and in mouse less than 1% of the 14C was present in the urine as aminocyclohexanols; unchanged cyclohexylamine accounted for about 95% of the activity. The extent of metabolism was not affected by either dose or route of administration. The species differences in metabolism may be implicated in the differences in toxicity during chronic high-dose administration.

摘要

给雄性小鼠和大鼠施用14C-环己胺(35 - 500毫克/千克)后,80%的14C剂量经尿液排出,大部分在给药后的头24小时内排出。在Wistar大鼠中,0 - 24小时尿液中的14C有7 - 9%以顺式-4-氨基环己醇的形式存在,其含量与相应的3-异构体相似。在DA大鼠中,尿液中以氨基环己醇形式存在的14C仅为1 - 2%,而在小鼠中,这一比例不到1%;未变化的环己胺约占活性的95%。代谢程度不受剂量或给药途径的影响。慢性高剂量给药期间的毒性差异可能与代谢的种属差异有关。

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