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三个非取代的类固醇构效关系的系统研究揭示11取代物具有高孕激素活性。鉴于 Desogestrel(17a-乙基-18-甲基-11-亚甲-4-雌烷-17-醇)对动物具有强的孕激素作用的活性,所以选用该药。在不同种属动物广泛研究了 desogestrel 的安全性;也研究了 desogestrel 与炔雌醇的结合应用。对妇女的安全性研究证明该药没有不良副作用。因此开始研究确定其既有良好避孕效果也能有效地控制周期的最低剂量的 Desogestrel/炔雌醇复合物。由于 desogestrel 的特殊性质,一个重要发现是,血浆性激素结合球蛋白(SHBG)对 Marve-
A systematic study of the structure-activity relationship of three unsubstituted steroids revealed that the 11 substituents have a high progestin activity. The drug was chosen because Desogestrel (17a-ethyl-18-methyl-11-methylene-4-estra-17-ol) has potent progestational activity in animals. The safety of desogestrel has been extensively studied in various species of animals; the combination of desogestrel with ethinylestradiol has also been studied. Studies on women’s safety have shown that the drug has no adverse side effects. Therefore, he started to study the lowest dose of Desogestrel / ethinyl estradiol complex which has been confirmed to have good contraceptive effect and cycle control. Due to the special nature of desogestrel, an important finding is that plasma levels of sex hormone binding globulin (SHBG) on Marve-