Response of rat ventral prostate to a new and novel 5 alpha-reductase inhibitor.

17β-N,N-Diethylcarbamoyl-4-methyl-4-aza-5αandrostan-3-one (4-MA) strongly inhibits the 5α-reductase-mediated conversion of testosterone (T) to 5α-dihydrotestosterone [17β-hydroxy-5α-androstan-3-one (DHT)] both in vitro and in vivo. In vitro, 4-MA is a more potent inhibitor than progesterone, androst-4-en-3-one-17β-carboxylic acid (17β), androst-4-en-3-one-17β-carboxylic acid methyl ester (17βME), megestrol acetate (17α-acetoxy-6-dehydro-6-methylprogesterone), medrogestone (6-methyl-6-dehydro-17-methylprogesterone), cyproterone acetate (17α-acetoxy-6-chloro-l,2α-methylene-4,5-pregnadiene-3,20-dione), or flutamide (4′-nitro-3′-trifluoromethylisobutyranilide). The effects of these compounds on prostatic concentrations of T and DHT were determined in young adult intact male rats treated 4 h before sacrifice. Subcutaneous injection of 0.33–10 mg 4-MAȯrat consistently reduced the prostatic concentrationof DHT but increased that of T. At 10 mg/rat, cyproterone acetate, megestrol acetate, and flutamide tended to ...

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