Komor A, Hobe G, Strecke J, Ponsold K, Grosse P, Goncharov N P, Schubert K
Zentralbl Gynakol. 1978;100(22):1454-8.
The interceptive activity of 2 new synthesized steroid compounds: STS 153 (17 beta-Phenylaminocarbonyloxy-estra-1,3,5(10)-triene-3-methyl ether and STS 287 (16 alpha-Bromo-17 beta-[N',N'-dimethylhydrazino]-carbonyloxy-estra-1,3,5(10)-triene-3-methyl ether) and of 17 alpha-Ethynylestradiol was investigated in baboons.--Postcoital oral administration of 1--3 mg/kg b. w. STS 153 for 5--7 days and of 1 mg/kg b. w. STS 287 for 5 days resulted in a fertility inhibition of about 90% and 95% respectively. A dose of 2 mg/kg b. w. of ethynylestradiol was necessary to attain complete fertility inhibition. Following administration of STS 153 and STS 287, side effects were not observed. Pharmacokinetic aspects are discussed.
研究了2种新合成的甾体化合物:STS 153(17β-苯氨基羰氧基-雌甾-1,3,5(10)-三烯-3-甲醚)和STS 287(16α-溴-17β-[N',N'-二甲基肼基]-羰氧基-雌甾-1,3,5(10)-三烯-3-甲醚)以及17α-乙炔雌二醇在狒狒中的避孕活性。——性交后口服1-3mg/kg体重的STS 153,持续5-7天,口服1mg/kg体重的STS 287,持续5天,分别导致约90%和95%的生育抑制。需要2mg/kg体重的乙炔雌二醇剂量才能实现完全生育抑制。给予STS 153和STS 287后,未观察到副作用。文中讨论了药代动力学方面的问题。