Mosbach E H, Shefer S, Abell L L
J Lipid Res. 1968 Jan;9(1):93-7.
17alpha-Methyltestosterone-4-(14)C was fed to two dogs in an experiment to determine tissue localization and metabolic disposition of this hypocholesterolemic steroid. No accumulation of the drug was found in any tissue, although a small amount of radioactivity was detected in the liver and the ileal mucosa of one animal. Most of the administered radio-activity was excreted in urine and feces. The urinary metabolites consisted largely of highly polar compounds which appeared resistant to glucuronidase treatment or solvolysis procedures. Analysis of the fecal metabolites showed the presence of unchanged methyltestosterone, of four isomeric methylandrostanediols, and of labeled unidentified polar compounds. Of the four identified methylandrostane-diols, the predominating fecal diols were 17alpha-methyl-5alpha-androstane-3beta,17beta-diol (45-62%) and 17alpha-methyl-5-androstane-3alpha,17-diol (12-28%); 17alpha-methyl-5alpha-androstane-3alpha,-17-diol and the 5beta:3beta isomer were found in very small amounts only.
在一项实验中，给两只狗投喂了17α-甲基睾酮-4-(14)C，以确定这种降胆固醇类固醇的组织定位和代谢情况。尽管在一只动物的肝脏和回肠黏膜中检测到少量放射性，但未在任何组织中发现药物蓄积。大部分给药放射性经尿液和粪便排出。尿液代谢产物主要由高度极性的化合物组成，这些化合物似乎对葡萄糖醛酸酶处理或溶剂分解程序具有抗性。粪便代谢产物分析显示存在未变化的甲基睾酮、四种异构甲基雄烷二醇以及标记的未鉴定极性化合物。在四种已鉴定的甲基雄烷二醇中，粪便中主要的二醇是17α-甲基-5α-雄烷-3β,17β-二醇（45 - 62%）和17α-甲基-5-雄烷-3α,17-二醇（12 - 28%）；仅发现极少量的17α-甲基-5α-雄烷-3α,-17-二醇和5β:3β异构体。
