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生物活性
Org30958 是體內(nèi)有效的芳香酶 (aromatase) 抑制劑。靶點(diǎn)
Aromatase
體內(nèi)研究
Besides inhibition of cornification of vaginal epithelium Org30958 (ORG 30958) decreases ovarian aromatase and plasma E2 levels in DHEAS-treated hypophysectomized rats. Plasma estradiol levels are also lowered by Org30958 in dogs which are treated with pregnant mare serum gonadotrophin in order to induce pro-estrus. Org30958 displays much less than 1/400th of the androgenic activity of testosterone propionate in immature castrated rats and appears to be devoid of estrogenic and anti-estrogenic activity in ovariectomized mature rats. A twice daily dose of 1.5 mg Org30958/kg postpones ovulation in mature female rats.