Effects of antiprostatic agents on 5.ALPHA.-dihydrotestosterone binding to rat hypophyseal and hypothalamic cytosol macromolecules.

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Abstract
The binding of 5.alpha.-dihydrotestosterone to the hypophyseal and hypothalamic cytosol macromolecules prepared from castrated male rats was observed. The effects of antiprostatic agents on 5.alpha.-dihydrotestosterone binding to both hypophyseal and hypothalamic cytosol macromolecules was examined. Cyproterone acetate and chlormadinone acetate showed the significant inhibiting effects on 5.alpha.-dihydrotestosterone binding to 7-8 S macromolecules of cytosol from both hypophyseal and hypothalamus. SCH 13521 [flutamide] and AA 560 [N-(2''-chloromethyl-2''-hydroxypropionyl)-3,4,5 trichloroaniline] did also affect 5.alpha.-dihydrotestosterone binding to 7-8 S macromolecules of cytosol from both tissues. An increasing number of steroidal and nonsteroidal antiandrogens have attracted the interest of investigators, because of their potential therapeutic use in prostatic cancer.