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THE ESTROGENIC ACTIVITIES OF 2-[3-ESTRONE-N-ETHYL-PIPERAZINE-METHYL]TETRACYCLINE(XW630) A NEW COMPOUND WITH ANTI-OSTEOPOROSIS ACTIVITY
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 9
- DOI:
- 10.3321/j.issn:0513-4870.1998.09.002
- Key Word:
- 四环素-哌嗪雌酚酮;雌激素受体;雌激素活性;抗骨质疏松作用
Abstract： 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.
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