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(3H)-5α-16-雄烯-3α-醇和(3H)-5α-16-雄烯-3-酮在人体内的代谢

The metabolism in man of (3H)-5alpha-16-androsten-3alpha-ol and of (3H)-5alpha-16-androsten-3-one.

作者信息

Kingsbury A E, Brooksbank B W

出版信息

Horm Res. 1978;9(5):254-70. doi: 10.1159/000178921.

Abstract

The in vitro metabolism in man of two 16-androstene steroids, 5alpha-16-androsten-3-one and 5alpha-16-androsten-3alpha-ol, has been studied using 3H-labelled tracers. 4 healthy subjects (2 of each sex) were chosen, and each labelled steroid was administered, by a single injection, to 1 man and 1 woman. Disappearance of (3H)-3alpha-androstenol in the subjects receiving this compound followed a curve which indicated a two-pool distribution in both cases; metabolic clearance rates for these subjects were found to be 3,790 1/24 h in the man and 3,120 1/24 h in the woman. Blood production rates calculated for the 3alpha-androstenol-treated subjects were 875 microgram/24 h in the man and 1,780 microgram/24 h in the woman. Recovery of 3H in the urine of all 4 subjects was very low, between 28 and 42%. Conversion of the injected precursors to urinary 3alpha-androstenol was 13.5 and 12.7% in the 2 men and 6.1 and 5.9% in the 2 women. The male subjects were found to have a lower 24-hour urinary 3alpha-androstenol output (570 and 387 microgram/24 h) than the average for men of their age. The urinary 3alpha-androstenol output in the women was 225 and 276 microgram/24 h, and was within the normal range for women. The urine production rates of 3alpha-androstenol were 2,470 and 4,090 microgram/24 h in the male and female subjects, respectively; the difference between the blood and urine production rates of this compound are thought to indicate the direct secretion of conjugates. Urine production rates of 5alpha-androstenone (measured as 3alpha-androstenol) were 2,370 and 4,340 microgram/24 h in the male and female subjects, respectively.

摘要

使用³H标记示踪剂,对两种16 - 雄烯类固醇(5α - 16 - 雄烯 - 3 - 酮和5α - 16 - 雄烯 - 3α - 醇)在人体中的体外代谢进行了研究。选取了4名健康受试者(男女各2名),每种标记类固醇通过单次注射分别给予1名男性和1名女性。接受该化合物的受试者体内(³H)-3α - 雄烯醇的消失遵循一条曲线,表明在两种情况下均呈现双池分布;这些受试者的代谢清除率在男性中为3790升/24小时,在女性中为3120升/24小时。经计算,接受3α - 雄烯醇治疗的受试者的血液生成率在男性中为875微克/24小时,在女性中为1780微克/24小时。所有4名受试者尿液中³H的回收率非常低,在28%至42%之间。在2名男性中,注射前体转化为尿中3α - 雄烯醇的比例分别为13.5%和12.7%,在2名女性中分别为6.1%和5.9%。发现男性受试者24小时尿中3α - 雄烯醇的排出量(570和387微克/24小时)低于其年龄组男性的平均水平。女性尿中3α - 雄烯醇的排出量为225和276微克/24小时,处于女性正常范围内。男性和女性受试者中3α - 雄烯醇的尿液生成率分别为2470和4090微克/24小时;该化合物血液和尿液生成率之间的差异被认为表明了结合物的直接分泌。男性和女性受试者中5α - 雄烯酮(以3α - 雄烯醇计)的尿液生成率分别为2370和4340微克/24小时。

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