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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0011,而雌酚酮与雌二醇分别为0325及1000。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
In order to find estrogen derivatives with small side effects and anti-osteoporosis, we used estrogen receptor binding inhibition assay, mouse vaginal cytology assay and young mice uterus weight method to study the effects of bone-targeting new compounds tetracycline Estrogenic activity of piperazine estrone (XW630). The results showed that the relative affinity of XW630 and estrogen receptor in uterine tissue was 0011, while the values of estrone and estradiol were 0325 and 1000, respectively. XW630 estrogen activity index and cytology experiments have shown that the estrogen activity of XW630 was significantly less than the estrone and estradiol. Suggesting that anti-osteoporosis activity of XW630 due to its low estrogen activity, it is worth further study