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本文研究了5α-双氢炔诺酮的性激素活性、抗着床作用及其机理。结果表明:该化合物有显著的抗孕激素作用,孕激素活性微弱。基本无雌激素活性,雄激素活性弱。10mg/kg 5α-双氢炔诺酮可完全抑制大鼠着床,并显著降低假孕大鼠卵巢静脉血孕酮水平。与大鼠子宫胞浆孕酮受体的相对结合亲和力(RBA)为孕酮的13％。其抗着床机理系在受体水平拮抗孕酮以及直接或间接抑制卵巢孕酮生物合成。
In this paper, 5α-dihydro norethindrone sex hormone activity, anti-implantation and its mechanism. The results show that: the compound has a significant anti-progesterone effect, progesterone activity was weak. Basically no estrogen activity, androgen activity is weak. 10mg / kg 5a-dihydro norethindrone can completely inhibit the implantation of rats, and significantly reduce the level of ovarian progesterone in pregnant rats. The relative binding affinity (RBA) to rat uterine cytosolic progesterone receptors was 13% of progesterone. Its anti-implantation mechanism antagonizes progesterone at the receptor level and directly or indirectly inhibits progesterone biosynthesis in the ovary.