【摘要】 为寻找副作用小而有抗骨质疏松作用的雌激素衍生物，用雌激素受体结合竞争抑制实验，小鼠阴道细胞学实验，幼雌小鼠子宫重量法分别研究了骨靶向新化合物四环素哌嗪雌酚酮（ＸＷ６３０）的雌激素活性。结果表明：ＸＷ６３０与子宫组织雌激素受体的相对亲和力为００１１，而雌酚酮与雌二醇分别为０３２５及１０００。ＸＷ６３０的雌激素活性指数及细胞学实验均表明ＸＷ６３０的雌激素活性明显小于雌酚酮及雌二醇。提示有抗骨质疏松活性的ＸＷ６３０由于其雌激素活性低，值得进一步研究更多还原

【Abstract】 2-[3-Estrone-N-ethyl-piperazine-methyl]tetracycline (XW630) showing antiosteoporosis activity is a new compound with piperazinetetracycline in the steroid structure of estrone. The affinity of XW630 with uterine estrogen receptor and its estrogenic activity were studied in this paper. The relative affinities of estrone, estradiol and XW630 with estrogen receptor (ER) of the uterine myoma tissues were found to be 0325,1000 and 0011, respectively, by the competitive assay. The estrogenic activity index of estrone, estradiol and XW630 were shown to be 970,1030 and 690, respctively, by the uterine weight assay using immature mice. These indexes indicate that: the estrogenic activity of XW630 is about 11960 that of estrone and 17742 that of estradiol. The vaginal smear assay of oophorectomized mice also showed that the estrogenic activity of XW630 is less than that of estrone and estradiol.更多还原