Lu Y C, Chatterton R T
Department of Obstetrics and Gynecology, Northwestern University Medical School, Chicago, Illinois 60611.
Adv Contracept. 1994 Jun;10(2):157-66. doi: 10.1007/BF01978109.
The purpose of this investigation was to determine the estrogenic and antiestrogenic activities of the potential contraceptive agent anordiol in the immature rat. A dose of 2.45 mumol of anordiol (AD), estradiol (E2), clomiphene citrate (CC), tamoxifen (TA), or the vehicle alone was administered to rats on the 25th and 29th days of age. Serum hormones were measured between 16:00 and 17:00 on days 30, 31, and 32; organ weights were determined on day 32. Anordiol and estradiol treatments significantly increased ovarian and uterine weight and serum LH concentrations, but CC and TA had no effect on these parameters. Vaginal cornification occurred before day 32 in all rats receiving anordiol or estradiol and in 3/5 and 4/5 rats receiving CC and TA, respectively, but not in control rats. Based on serum progesterone levels, ovulation was induced only in rats receiving anordiol or estradiol. All of the compounds tested significantly increased serum testosterone above levels in control animals, but both AD and E2 induced ovulation without a further increase in serum testosterone. We conclude that in the immature rat anordiol produces estrogenic responses in the vagina, uterus and in the hypothalamic-pituitary-ovarian axis, whereas TA and CC are estrogenic only on the vaginal and uterine epithelium.
本研究的目的是确定潜在避孕药炔诺醇在未成熟大鼠体内的雌激素活性和抗雌激素活性。在大鼠25日龄和29日龄时，分别给予2.45 μmol的炔诺醇（AD）、雌二醇（E2）、枸橼酸氯米芬（CC）、他莫昔芬（TA）或仅给予溶剂。在30、31和32日龄的16:00至17:00之间测定血清激素水平；在32日龄时测定器官重量。炔诺醇和雌二醇处理显著增加了卵巢和子宫重量以及血清促黄体生成素浓度，但CC和TA对这些参数没有影响。在32日龄前，所有接受炔诺醇或雌二醇的大鼠以及分别接受CC和TA的3/5和4/5大鼠出现了阴道角化，但对照大鼠未出现。根据血清孕酮水平，仅接受炔诺醇或雌二醇的大鼠诱导排卵。所有测试化合物均使血清睾酮水平显著高于对照动物，但AD和E2在未进一步增加血清睾酮的情况下诱导排卵。我们得出结论，在未成熟大鼠中，炔诺醇在阴道、子宫以及下丘脑-垂体-卵巢轴产生雌激素反应，而TA和CC仅在阴道和子宫上皮具有雌激素作用。
