The effects of antioestrogens, antiandrogens and of various inhibitors of testosterone metabolism on testosterone metabolism in the quail hypothalamus and cloacal gland were studied by an in-vitro radio-enzymatic assay. It was found that antioestrogens and antiandrogens generally had little or no effect on aromatase and 5α- and 5β-reductases of testosterone, except when used at very high doses. The 5α-reductase inhibitor, 17β-N,N-diethylcarbamoyl-4-methyl-4-aza-5α-androstan-3-one, inhibited both 5α- and 5β-dihydrotestosterone production without markedly affecting aromatase activity. Surprisingly, the aromatase inhibitor, 1,4,6-androstatriene-3,17-dione, inhibited not only the production of oestradiol but also that of 5β-dihydrotestosterone and, to a lesser extent, 5α-dihydrotestosterone. These unexpected properties should be taken into account when interpreting the results of in-vivo experiments using these compounds.
J. Endocr. (1987) 112, 189–195