Wright D J, Robinson H K, Holder G M, Ryan A J, Bonin A M, Baker R S
Xenobiotica. 1985 Oct;15(10):825-34. doi: 10.3109/00498258509045034.
The biliary excretion of radioactivity by adult Wistar rats given i.v. 7-methyl-[7-14C]benz[c]acridine(14C-7-MBAC) and [methyl-3H]-7-methylbenz[c]acridine (3H-7-MBAC) (2 mg/kg) was 61% and 48%, respectively, in males in six hours. Females excreted 33% of a 2 mg/kg dose of 3H-7-MBAC in the same time-period. For male rats, the urinary and faecal excretions were about 10% and 61% of the dose of 14C-7-MBAC, respectively, in seven days. No enterohepatic circulation could be demonstrated in control male rats. The biliary excretion of radioactivity by phenobarbital- and 3-methylcholanthrene-induced male rats given 14C-7-MBAC was similar to or greater than that of control male rats. The organo-soluble biliary metabolites after beta-glucuronidase/arylsulphatase hydrolysis were separated by h.p.l.c., and quantitative metabolite distributions were obtained for induced and control rats by comparison with metabolite standards. The mutagenicity of bile from carcinogen-dosed control rats was greater than that of equivalent bile from carcinogen-dosed 3-methylcholanthrene-pretreated animals.
静脉注射给予成年Wistar大鼠2毫克/千克的7-甲基-[7-¹⁴C]苯并[c]吖啶（¹⁴C-7-MBAC）和[甲基-³H]-7-甲基苯并[c]吖啶（³H-7-MBAC）后，雄性大鼠在6小时内放射性物质的胆汁排泄率分别为61%和48%。雌性大鼠在相同时间段内排泄了2毫克/千克剂量³H-7-MBAC的33%。对于雄性大鼠，在7天内，¹⁴C-7-MBAC剂量的尿液和粪便排泄率分别约为10%和61%。在对照雄性大鼠中未发现肠肝循环。给予¹⁴C-7-MBAC的苯巴比妥和3-甲基胆蒽诱导的雄性大鼠放射性物质的胆汁排泄与对照雄性大鼠相似或更高。经β-葡萄糖醛酸酶/芳基硫酸酯酶水解后的有机可溶性胆汁代谢物通过高效液相色谱法分离，并通过与代谢物标准品比较获得诱导和对照大鼠的定量代谢物分布。给予致癌物的对照大鼠胆汁的致突变性大于给予致癌物的3-甲基胆蒽预处理动物的等量胆汁。
