Yamashita S, Ohno Y, Watanabe Y, Fujimoto Y, Koishi K, Kawashima M, Hosokawa K, Okada H
Department of Obstetrics and Gynecology, Kyoto Prefectural University of Medicine, Japan.
Gynecol Obstet Invest. 1994;38(4):245-8. doi: 10.1159/000292490.
To examine antiestrogenic effects of danazol through the receptor system and to clarify its direct effects on the endometrium in vivo, we applied danazol jelly directly into the rabbit uterine cavity and measured uterine estrogen, progesterone and androgen receptors (ER, PR and AR, respectively). Danazol significantly reduced ER, PR and AR (p < 0.05). Treatment with receptor-blocking agents (RU 486 and oxendolone) showed that the decrease in the ER level showed a closer association with that in PR than with AR. These results indicate that danazol directly administered into the uterine cavity is absorbed by the endometrial tissue and exerts its antiestrogenic effects possibly through PR in the cells.
为了通过受体系统研究达那唑的抗雌激素作用,并阐明其在体内对子宫内膜的直接作用,我们将达那唑凝胶直接应用于兔子宫腔内,并测量子宫雌激素、孕激素和雄激素受体(分别为ER、PR和AR)。达那唑显著降低了ER、PR和AR(p<0.05)。用受体阻断剂(RU 486和氧雄龙)治疗表明,ER水平的降低与PR的降低比与AR的降低关系更密切。这些结果表明,直接注入子宫腔的达那唑被子宫内膜组织吸收,并可能通过细胞内的PR发挥其抗雌激素作用。