3－酮－地索高诺酮对雌、孕及雄激素受体亲和力选择性的实验研究

采用体外放射配体受体结合法测定３－酮－地索高诺酮（ＫＤＧ）与兔子宫胞浆雌激素受体（ＥｃＲ）、孕激素受体（ＰｃＲ）和大鼠腹侧前列腺胞浆雄激素受体（ＡｃＲ）结合的亲和力，并以左旋１８－甲基炔诺酮（ＬＮＧ）作对照，从受体水平探讨ＫＤＧ对当体激素受体的选择性。结果表明：ＫＤＧ对ＰｃＲ有很高的亲和力，是ＬＮＧ的１．５倍；对ＡｃＲ的亲和力很低，仅为ＬＮＧ的０．７４倍；对ＥｃＲ几乎没有亲和力，受体亲和力选择系数也明显高于ＬＮＧ。由此可见，在ＬＮＧ甾核结构中Ｃ１１位引入次甲基合成的ＫＤＧ，其受体亲和力选择性更专一。

Studies on the binding affinity of 3-keto-desogestrel with estrogen,progcstogen and androgen receptors

Radio-ligand binding assay(RLBA)in vitro was applied to measure the relative bindingaffinity(RBA)of 3-keto-desogestrel(KDG) with estrogen and progestogen receptors (EcR、 PcR)inrabbit uterine cytosol and androgen receptor(AcR)in rat ventral prostate cytosol,in com=p,drisoii xvI tlilevonorgestrel(LNG)。 ResuIts indicated that RBA of KDG for PcR was very high, which was 1.5 timesthat of LNG;RBA of KDG for AcR was low,wmch was0.74times than that of LNG;KDG had almostunmeasurable affinity for EcR。 Selectivity index for receptor affinity (RBA-PcR/RBA-AcR) of KDGwas remarkably higher than that of LNG。It is suggested that KDG would be a more specific progestogenthan LNG by the addition of methylene at the position of C11 of steroid ring。