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

R L Barbieri, Robert L. Barbieri, Hanmin Lee, H. Lee, Kenneth J. Ryan, K J Ryan
Fertility and sterility · 1979 · vol. 31(2) , pp. 182–186 · doi:10.1016/s0015-0282(16)43820-3 · PMID:761680 · W2409283123
Lab / animal OA: closed CC0 ⤵ 72 in-corpus citations
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This study investigated the binding affinities of danazol to rat androgen, glucocorticoid, progesterone, and estrogen receptors and correlated these findings with the drug's known biological activity.

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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.

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MeSH descriptors

Danazol Pregnadienes Receptors, Glucocorticoid Receptors, Steroid Animals Danazol Dihydrotestosterone Dihydrotestosterone Female Male Mestranol Mestranol Methyltestosterone Methyltestosterone Pregnadienes Rats Receptors, Estrogen Receptors, Estrogen Receptors, Glucocorticoid Receptors, Progesterone

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