Lax E R, Kreuzfelder E, Schriefers H
Steroids. 1980 Nov;36(5):521-9. doi: 10.1016/0039-128x(80)90075-6.
5 alpha-Dihydrotestosterone, 17-hydroxyprogesterone caproate, 2-methoxyestrone and a number of nonsteroidal antiestrogens (clomiphene citrate, nafoxidine hydrochloride, tamoxifen, MER-25) were tested for their ability to block estradiol-mediated repression of the androgen-dependent 3 beta-hydroxysteroid dehydrogenase activity of male rat liver. With the exception of 5 alpha-dihydrotestosterone, which induced activity in females, none of these substances affected 3 beta-hydroxysteroid dehydrogenase activity when administered alone to otherwise untreated male and female rats. Tamoxifen (100 or 500 micrograms/day) was the only substance which prevented a decrease in enzyme activity when given simultaneously with estradiol (5 micrograms/day). The estradiol-mediated decrease in activity was not antagonized by a 100-fold higher dose of androgen (5 alpha-dihydrotestosterone, 0.5 mg/day), demonstrating the potent antiandrogenic effect of estradiol on this hepatic androgen-dependent enzyme activity.
对5α-双氢睾酮、己酸17-羟孕酮、2-甲氧基雌酮以及多种非甾体类抗雌激素药物（枸橼酸氯米芬、盐酸萘福昔定、他莫昔芬、MER-25）进行了测试，以考察它们阻断雌二醇介导的对雄性大鼠肝脏雄激素依赖性3β-羟基类固醇脱氢酶活性抑制作用的能力。除了在雌性大鼠中诱导该酶活性的5α-双氢睾酮外，当将这些物质单独给予未经处理的雄性和雌性大鼠时，没有一种物质会影响3β-羟基类固醇脱氢酶的活性。他莫昔芬（100或500微克/天）是唯一一种在与雌二醇（5微克/天）同时给药时能阻止酶活性降低的物质。雌二醇介导的活性降低并未被剂量高100倍的雄激素（5α-双氢睾酮，0.5毫克/天）所拮抗，这表明雌二醇对这种肝脏雄激素依赖性酶活性具有强大的抗雄激素作用。
