Fiala E S, Stathopoulos C
J Cancer Res Clin Oncol. 1984;108(1):129-34. doi: 10.1007/BF00390984.
The basic parameters of the metabolism of methylazoxymethanol-(N,N'-methyl-14C) acetate, in terms of exhaled 14CO2, urinary metabolites, and inhibition by pyrazole and disulfiram, were examined in F344 rats and strain-2 guinea pigs. After a 18.7 mg/kg SC dose, 45% (6 h) and 49.5% (24 h) was exhaled as 14CO2, and 6.6% (24 h) of the radioactivity was excreted in the urine by the rats. After identical treatment, 36.5% (6 h) and 39.5% (24 h) was exhaled as 14CO2 and 3.5% (24 h) was excreted in the urine by the guinea pigs. Urea-14C and methylazoxymethanol(-14C) were the major urinary metabolites. In both species, pretreatment with pyrazole (40 or 360 mg/kg, IP) caused a significant reduction of exhaled 14CO2 and an increase in the amount of urinary methylazoxymethanol(-14C). Similar but less pronounced effects were observed after pretreatment of rats with disulfiram (1 g/kg, PO). These results are discussed with respect to possible enzyme systems involved in the metabolic activation of methylazoxymethanol in vivo.
在F344大鼠和2系豚鼠中，根据呼出的14CO2、尿液代谢产物以及吡唑和双硫仑的抑制作用，研究了甲基偶氮甲醇-（N，N'-甲基-14C）乙酸酯的代谢基本参数。经皮下注射18.7mg/kg剂量后，大鼠呼出的14CO2分别占45%（6小时）和49.5%（24小时），放射性的6.6%（24小时）通过尿液排出。经相同处理后，豚鼠呼出的14CO2分别占36.5%（6小时）和39.5%（24小时），3.5%（24小时）通过尿液排出。尿素-14C和甲基偶氮甲醇（-14C）是主要的尿液代谢产物。在两个物种中，用吡唑（40或360mg/kg，腹腔注射）预处理均导致呼出的14CO2显著减少，尿液中甲基偶氮甲醇（-14C）的量增加。用双硫仑（1g/kg，口服）预处理大鼠后观察到类似但不太明显的效果。针对体内甲基偶氮甲醇代谢活化可能涉及的酶系统对这些结果进行了讨论。
