Danazol suppression of luteinizing hormone secretion: a role for danazol-androgen receptor interaction within the brain-pituitary complex

In: Fertility and Sterility · 1981 · vol. 35(4) , pp. 467–472 · doi:10.1016/s0015-0282(16)45446-4 · PMID:7215573 · W2463221644
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This study investigated how danazol suppresses luteinizing hormone secretion by examining the interaction between danazol and androgen receptors in the brain and pituitary gland.

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Abstract

We investigated the relationship between intracellular androgen and estrogen receptors within the brain-pituitary complex and danazol suppression of luteinizing hormone secretion in castrated rats. Danazol did not influence 3H-estradiol-estrogen receptor interactions within the brain and pituitary but did suppress 3H-dihydrotestosterone-androgen receptor interactions within this neuroendocrine complex. To study the significance of these danazol-androgen receptor interactions, the drug was administered to androgen receptor-deficient pseudohermaphrodite or flutamide-treated male rats. In both instances, danazol suppression of luteinizing hormone release was markedly attenuated or absent. These findings point to danazol-androgen receptor interactions within the brain-pituitary complex as a key step in this drug's antigonadotropic actions. Whether the active drug form is danazol itself or a metabolite is subject to further study.

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