Lingg R D, Kaylor W H, Pyle S M, Kopfler F C, Smith C C, Wolfe G F, Cragg S
Drug Metab Dispos. 1982 Mar-Apr;10(2):134-41.
1,2,4-Trichloro[14C]benzene (TCB) was administered po (10 mg/kg) and iv (10 mg/kg) to rats and rhesus monkeys. Urine was collected at 24 hr and the major urinary metabolites were quantified and identified. By 24 hr, the monkey had excreted 22% of the iv dose and roughly 40% of the po dose in the urine. Less than 1% of the radioactivity was found in the monkey's feces. An isomeric pair of 3,4,6-trichloro-3,5-cyclohexadiene-1,2-diol glucuronides accounted for between 48 and 61% of the urinary metabolites. Glucuronides of 2,4,5- and 2,3,5-trichlorophenol (TCP) accounted for 14 to 37%, and unconjugated TCP's accounted for 1-37% of the monkey's urinary metabolites. For the rat, 84% of the po dose and 78% of the iv dose were collected in the urine by 24 hr; 11% and 7%, respectively, were the amounts collected in the feces. Two isomers, 2,4,5- and 2,3,5-, of N-acetyl-S-(trichlorophenyl)-L-cysteine accounted for 60-62% of the rat's urinary metabolites. Free 2,4,5- and 2,3,5-isomers of trichlorothiophenol amounted to 33% of the urinary metabolites in the po dosed rats and 28% in the iv dosed rats; free 2,4,5- and 2,3,5-TCP's amounted to 1% and 10%, respectively. These results show that there is a sharp division in the types of conjugates formed in the metabolism of 1,2,4-TCB by the rat and rhesus monkey.
给大鼠和恒河猴经口（10毫克/千克）和静脉注射（10毫克/千克）给予1,2,4-三氯[¹⁴C]苯（TCB）。在24小时收集尿液，并对主要尿代谢物进行定量和鉴定。到24小时时，猴子经静脉注射剂量的22%以及经口剂量的约40%已通过尿液排出。在猴子粪便中发现的放射性物质不到1%。一对3,4,6-三氯-3,5-环己二烯-1,2-二醇葡萄糖醛酸异构体占尿代谢物的48%至61%。2,4,5-和2,3,5-三氯苯酚（TCP）的葡萄糖醛酸酯占猴子尿代谢物的14%至37%，未结合的TCP占1%至37%。对于大鼠，到24小时时，经口剂量的84%和静脉注射剂量的78%通过尿液收集；粪便中收集的量分别为11%和7%。N-乙酰-S-（三氯苯基）-L-半胱氨酸的两种异构体2,4,5-和2,3,5-占大鼠尿代谢物的60%至62%。在经口给药的大鼠中，三氯硫酚的游离2,4,5-和2,3,5-异构体占尿代谢物的33%，在静脉注射给药的大鼠中占28%；游离2,4,5-和2,3,5-TCP分别占1%和10%。这些结果表明，大鼠和恒河猴在1,2,4-TCB代谢过程中形成的结合物类型存在明显差异。
