Braasch H V, Frederiksen M C, Chatterton R T
Department of Obstetrics and Gynecology, Northwestern University Medical School, Chicago, IL 60611.
Steroids. 1988 Sep;52(3):279-94. doi: 10.1016/0039-128x(88)90009-8.
[4-14C]Progesterone was administered to two cycling female monkeys during the luteal phase of the cycle, and blood and urine were sampled over a 24 h period. Progesterone had a volume of distribution of 1.75 +/- 0.3 L/kg, and a plasma elimination clearance of 0.06 +/- 0.03 L/kg/min. In comparison to the human, plasma progesterone binding was greater and progesterone clearance was slower in the cynomolgus monkey. The major unconjugated metabolite in plasma was 20 alpha-hydroxy-4-pregnen-3-one. In urine 6.2% of 14C-steroids were unconjugated, 2.3% of which were [14C]progesterone. Thin-layer chromatography (TLC) of conjugated metabolites in urine revealed that 24% had the mobility of sulfates, 19% that of glucuronides, and 52% were more polar. After hydrolysis of conjugates, a major fraction chromatographed with pregnanediol. However, despite evidence for the presence of a 20 alpha-hydroxyl group, none of the pregnanediol isomers could be identified among these 14C-steroids. Nevertheless, over 80% of urinary metabolites had sufficient analogy to pregnanediol to bind to an antiserum specific for ring D and the C-17 side-chain of pregnanediol.
在黄体期，给两只处于月经周期的雌性猕猴注射了[4-¹⁴C]孕酮，并在24小时内采集血液和尿液样本。孕酮的分布容积为1.75±0.3L/kg，血浆清除率为0.06±0.03L/kg/min。与人类相比，食蟹猴血浆中孕酮结合力更强，孕酮清除更慢。血浆中主要的未结合代谢物是20α-羟基-4-孕烯-3-酮。尿液中6.2%的¹⁴C-类固醇是未结合的，其中2.3%是[¹⁴C]孕酮。尿液中结合代谢物的薄层色谱分析（TLC）显示，24%具有硫酸盐的迁移率，19%具有葡萄糖醛酸苷的迁移率，52%极性更强。结合物水解后，大部分与孕二醇一起进行色谱分析。然而，尽管有证据表明存在20α-羟基基团，但在这些¹⁴C-类固醇中未能鉴定出任何孕二醇异构体。尽管如此，超过80%的尿液代谢物与孕二醇有足够的相似性，能够与针对孕二醇D环和C-17侧链的抗血清结合。
