安今益上市会外国教授演讲稿.pptVIP

all absolute DFs for 屈螺酮 were 显著 greater than 1 屈螺酮 was characterized by一种favorable 区分 of 子宫和乳腺 作用 in vivo 屈螺酮 had 子宫 活性 at 剂量 低er than those that were efficacious in the 乳腺 Conversely, 屈螺酮 显示 显著 greater 区分 (6-到33-倍) of 子宫 与 相比 增殖 乳腺 作用 when compared with MPA Comparing the relative DFs measuring 增殖 活性, 屈螺酮 显示 显著 greater 区分 (6-到33-倍) of 子宫 与 相比 增殖 乳腺 作用 than MPA In comparison with MPA, 屈螺酮 显示一种superior in vivo profile with regard到区分 of 子宫和增殖 乳腺 作用. 屈螺酮, but not MPA, appears到offer一种安全性 window 之间 子宫 孕激素的 活性和增殖 乳腺 作用. The explanation for the favorable 区分 of 子宫 与 相比 增殖 乳腺 作用 seen with 屈螺酮, but not with MPA,是uncertain. Possible explanations: 不同 PR ligands induce 不同 PR conformations that have variable 影响s on PR/cofactor interaction和thus 基因 表达 in PR target tissues. If this是correct, it would not be surprising that MPA和屈螺酮 have diverse 作用, 即使通过 they act on 相同的receptor. Both MPAand 屈螺酮 bind to和activate the PR, but they also 发挥 additional activities on其他nuclear receptors. Notably, MPA has significant glucocorticoid 活性, whereas 屈螺酮是inactive at the GR but behaves as strong 抗盐皮质激素. It是tempting到speculate that the glucocorticoid 活性 of MPA that是lacking for 屈螺酮 provoked the enhanced mitogenic 活性 of MPA in the 乳腺 under our experimental conditions. it has been suggested that the 盐皮质激素 receptor可以compensate for GR 功能 within the 乳腺. It可能be hypothesized that both glucocorticoid和盐皮质激素 活性 enhance the proliferation proliferation of mammary epithelial 细胞. Based on this theory, the 抗盐皮质激素 活性 of 屈螺酮 could contribute到its reduced 增殖 活性 in the 乳腺 when compared with MPA 安今益_04.ppt * * favorable 区分 of 子宫和乳腺 作用 in vivo 子宫 活性 at 剂量 低er than those that were efficacious in the 乳腺 MPA was equally active in the uterus和the 乳腺 at 相同的剂量 Comparing the relative DFs measuring 增殖 活性, 屈螺酮 显示 显著 greater 区分 (6-到33-倍) of 子宫 与 相比 增殖 乳腺 作用 than MPA 安今益_04.ppt * * * § Gambacciani M, et al. In preparation 服用钙 (对照组)或1 mg 17β-雌二醇 (E2) + 2 mg 屈螺酮 (DRSP) (E2 + DRSP) 对收缩压的影响 *P 0.001和§ P 0.0069 与 相比 相应的基础 水平 血压降低对绝经后妇