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• W2021120441 abstract "Somewhat surprisingly in view of its chemical constitution, SCH 13521 antagonises the biological activity of testosterone in vivo in a manner reminiscent of the steroid-related anti-androgen, cyproterone acetate. Accordingly, SCH 13521 severely curtails the nuclear binding of 5α-dihydrotestosterone in the accessory sexual glands when administered in vivo and also counters the testosteronemediated stimulation of RNA polymerase activity. In sharp contrast, SCH 13521 was a singularly less effective anti-androgen when measured under experimental conditions in vitro. In measurements conducted in cell-free systems, SCH 13521 failed to prevent the high affinity binding of 5α-dihydrotestosterone under conditions where cyproterone acetate fully retained its anti-androgenic activity. In view of the disparity between the activity of this non-steroidal anti-androgen measured under conditions in vivo as against in vitro, it is concluded that SCH 13521 may have to undergo obligatory metabolism to a more active compound before its anti-androgenic properties are manifest. The nature of this metabolite remains to be established. As in the case of cyproterone acetate, there was no convincing evidence to suggest that SCH 13521 impairs the metabolism of testosterone in the accessory sexual glands." @default.
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• W2021120441 date "1974-04-01" @default.
• W2021120441 modified "2023-09-27" @default.
• W2021120441 title "An investigation into the anti-androgenic properties of the non-steroidal compound, sch 13521 (4′-nitro-3′-trifluoromethylisobutyrylanilide)" @default.
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• W2021120441 doi "https://doi.org/10.1016/0303-7207(74)90004-5" @default.
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