Stanley S M, Smith L, Rodgers J P
Jockey Club of Southern Africa, Johannesburg, Gauteng, Republic of South Africa.
J Chromatogr B Biomed Sci Appl. 1997 Mar 7;690(1-2):55-64. doi: 10.1016/s0378-4347(96)00404-5.
The metabolism of the orally active anabolic steroid methyltestosterone in the equine was investigated by administration of the drug along with a tritiated radiolabel tracer. In this study some of the metabolites were identified and a radio immunoassay screen and immunoaffinity chromatography gel for methyltestosterone were also evaluated. Pathway intermediates, in particular the 17-methylandrostanediols, were studied to gain an insight into the most likely stereochemistry of the major metabolites. The predominant phase I biotransformations involve reduction of the A ring 3-oxo and 4-ene groups to yield predominantly 3 beta-hydroxy-5 alpha-androstane products and hydroxylation of the steroid nucleus at several positions. Epimerisation of the 17 alpha-methyl group also occurred. Ten steroids could be positively identified by comparison with authentic reference materials and many other triol, tetrol and pentols were also observed. Phase II metabolites and sulphate conjugates in particular, were common.
通过给予药物并伴随氚标记的放射性示踪剂，研究了口服活性合成代谢类固醇甲基睾酮在马体内的代谢情况。在本研究中，鉴定了一些代谢物，还评估了甲基睾酮的放射免疫分析筛选和免疫亲和色谱凝胶。对途径中间体，特别是17-甲基雄烷二醇进行了研究，以深入了解主要代谢物最可能的立体化学。主要的I相生物转化包括A环3-氧代和4-烯基的还原，主要产生3β-羟基-5α-雄烷产物，以及类固醇核在多个位置的羟基化。17α-甲基也发生了差向异构化。通过与真实参考物质比较，可以明确鉴定出10种类固醇，还观察到许多其他的三醇、四醇和戊醇。特别是II相代谢物和硫酸盐结合物很常见。
