达那唑与大鼠雄激素、糖皮质激素、孕激素及雌激素受体的结合：与生物活性的相关性。

Danazol binding to rat androgen, glucocorticoid, progesterone, and estrogen receptors: correlation with biologic activity.

作者信息

Barbieri R L, Lee H, Ryan K J

出版信息

Fertil Steril. 1979 Feb;31(2):182-6. doi: 10.1016/s0015-0282(16)43820-3.

Abstract

Danazol was found to possess androgenic and glucocorticoid activity in rat bioassays. In contrast, danazol displayed no significant estrogenic activity. In support of these findings, danazol bound to the 8 S androgen receptor of rat prostate cytosol and to the glucocorticoid receptor of rat liver cytosol, but danazol did not bind well to the estrogen receptor of the rat uterus. Finally, danazol bound to the progesterone receptor of the rat uterus, but controversy continues as the whether danazol possesses progestational, antiprogestational, or no progestational effects.

摘要

在大鼠生物测定中发现达那唑具有雄激素和糖皮质激素活性。相比之下，达那唑没有显著的雌激素活性。为支持这些发现，达那唑与大鼠前列腺细胞质的8S雄激素受体以及大鼠肝脏细胞质的糖皮质激素受体结合，但达那唑与大鼠子宫的雌激素受体结合不佳。最后，达那唑与大鼠子宫的孕激素受体结合，但关于达那唑是否具有孕激素、抗孕激素或无孕激素作用仍存在争议。