Hobe G, Bartels F, Schubert K
Endokrinologie. 1976 Jul;67(3):282-8.
The sulfate and phosphate conjugates of 19-nortestosterone (17beta-hydroxy-estr-4-ene-3-one) and ent-19-nortestosterone (ent-17beta-hydroxy-estr-4-ene-3-one) have been synthesized. The sodium salts of the conjugates were i.v. infused to 2 women. On days 1--4 following application, the 19-nortestosterone and 17-ketosteroid excretion in urine as well as the 19-nortestosterone conjugation have been estimated. The 19-nortestosterone enantiomers were excreted in nearly the same amounts. In comparison to testosterone, the excretion of unchanged steroid (20--50%) is significantly higher. The sulfate conjugates of the enantiomers are not hydrolyzed in vivo, whereas the phosphate conjugates are completely splitted. Hydrolysis of ent-nortestosterone phosphate takes place obviously more slowly. Urinary 17-ketosteroids are significantly increased only following infusion of 19-nortestosterone phosphate.
已合成了19-去甲睾酮(17β-羟基-雌-4-烯-3-酮)和对映体19-去甲睾酮(对映体17β-羟基-雌-4-烯-3-酮)的硫酸盐和磷酸盐共轭物。将共轭物的钠盐静脉注射给2名女性。在应用后的第1 - 4天,对尿中19-去甲睾酮和17-酮类固醇的排泄以及19-去甲睾酮的共轭作用进行了评估。19-去甲睾酮对映体的排泄量几乎相同。与睾酮相比,未变化类固醇的排泄量(20 - 50%)明显更高。对映体的硫酸盐共轭物在体内不被水解,而磷酸盐共轭物则完全分解。对映体19-去甲睾酮磷酸盐的水解明显更慢。仅在注射19-去甲睾酮磷酸盐后,尿中17-酮类固醇显著增加。