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• W2043284600 abstract "Summary. objective The influence of ketoconazole on the various enzymes of human adrenal steroid biosynthesis was examined in vitro. measurements After Incubation of human adrenal tissue slices with labelled precursors and ketoconazole (0–2000 μM), radioactive metabolites were separated by thin-layer chromatography and quantified by liquid scintillation counting. Enzyme activity was assessed by measuring conversion of tritium-labelled precursors to products. results In vitro, ketoconazole showed a significant Inhibition on the following adrenal enzyme systems (with decreasing activity): C17,20-desmolase (IC50 2 μM), 16α-hydroxylase (IC50 9 μM), 17α-hydroxylase (IC50 18 μM), 18-hydroxylase (IC50 28 μM), and 11 β-hydroxylase (IC50 35 μM). In the tested concentrations ketoconazole had no Inhibitory effect on the 21-hydroxylase, the 3β-hydroxysteroid dehydrogenase and the 20-hydroxysteroid dehydrogenase component of the C17,20-desmolase enzyme system. conclusions The data are in accordance with clinical findings where a strong suppression of serum androgen levels by relatively selective inhibition of C17,20-desmolase has been assumed. The predominant blocking effect of ketoconazole on adrenal as well as on gonadal androgen biosynthesis might be of clinical benefit in the management of hyperandrogenic states." @default.
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• W2043284600 date "1991-08-01" @default.
• W2043284600 modified "2023-10-14" @default.
• W2043284600 title "The influence of ketoconazole on human adrenal steroidogenesis: incubation studies with tissue slices" @default.
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• W2043284600 doi "https://doi.org/10.1111/j.1365-2265.1991.tb03516.x" @default.
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