Studies on the mechanism of action of danazol and gestrinone (R2323) in the rat: evidence for a masked estrogen component*

B. W. Snyder, G. D. Beecham, Richard C. Winneker
In: Fertility and Sterility · 1989 · vol. 51(4) , pp. 705–710 · doi:10.1016/s0015-0282(16)60625-8 · PMID:2466705 · W113465115
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This study investigated the mechanisms of action for danazol and gestrinone in rats, finding evidence that gestrinone possesses a masked estrogen component.

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Abstract

The effects of androgen and estrogen receptor antagonists on the action of danazol and gestrinone (R2323) were investigated. The tropic effect of danazol and gestrinone on sex accessory tissues of castrated, immature male rats was inhibited by the antiandrogen flutamide, whereas the uterotropic action of these steroids in immature female and adult ovariectomized rats was not inhibited by flutamide. In contrast, the uterotropic effect of danazol was reduced by the antiestrogen, LY156758. The estrogen-sensitive endpoints, vaginal keratinization and uterine progesterone receptor concentration, were enhanced by treatment with a combination of flutamide and either danazol or gestrinone. These data indicate that danazol and gestrinone have estrogenic activity that is masked by the androgenic component of these drugs.

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