Koch R L, Rose C, Rich T A, Goldman P
Biochem Pharmacol. 1982 Feb 1;31(3):411-4. doi: 10.1016/0006-2952(82)90190-3.
The metabolism of the radiation sensitizer misonidazole was similar in anaerobic cecal contents and hypoxic Chinese hamster lung fibroblasts (V-79-473). Both systems formed the amino derivative of misonidazole, [1-(2-aminoimidazol-1-yl)-3-methoxypropan-2-ol] (AIM), and urea, as well as a metabolite, (2-hydroxy-3-methoxypropyl)-guanidine (G), which has not been described previously. It appears that the nitro group of misonidazole was reduced to form AIM and that this compound was then hydrolyzed to yield either urea or G, the latter in yields of 25% (tissue culture) to 55% (cecal contents). When tested with the Ames tester strain, both G and AIM were slightly mutagenic only for strain TA 98 and then only in the presence of the system for microsomal activation.
放射增敏剂米索硝唑在厌氧盲肠内容物和缺氧的中国仓鼠肺成纤维细胞（V - 79 - 473）中的代谢情况相似。这两个系统都形成了米索硝唑的氨基衍生物，即[1 - (2 - 氨基咪唑 - 1 - 基)-3 - 甲氧基丙 - 2 - 醇]（AIM）和尿素，以及一种此前未被描述过的代谢物，(2 - 羟基 - 3 - 甲氧基丙基)-胍（G）。看来米索硝唑的硝基被还原形成AIM，然后该化合物被水解生成尿素或G，后者的产率在25%（组织培养）至55%（盲肠内容物）之间。当用艾姆斯试验菌株进行测试时，G和AIM仅对TA 98菌株有轻微致突变性，且仅在存在微粒体激活系统时才会如此。
