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Trilostane is a competitive inhibitor of 3beta-hydroxysteroid dehydrogenase. In vitro, the drug inhibits conversion of pregnenolone to progesterone but does not alter conversion of cholesterol to pregnenolone nor progesterone to corticoid hormones. When given orally to rats, trilostane inhibits corticosterone and aldosterone production and elevates… (More)
Trilostane inhibits adrenal, ovarian, and placental steroidogenesis when administered orally to rhesus monkeys. By inhibiting 3 beta-hydroxysteroid dehydrogenase activity, it causes an increase in circulating levels of pregnenolone. Trilostane reverses the stimulation of luteal progesterone production and the delay in onset on menstruation induced by human… (More)
The synthetic steroid nivazol lacks three of the substituents considered to be important for glucocorticoid activity, i.e. the 3-keto, the 11-hydroxy, and the 20-keto groups. Nevertheless, in the rat, nivazol has the activity profile of a glucocorticoid. After treatment of intact female rats with nivazol , the mean weights of the adrenals and thymus were… (More)
1. Aerobic incubation of [(14)C]oestradiol, in the presence of surviving gut tissue of the sea urchin Strongylocentrotus franciscanus, or a soluble enzyme system prepared therefrom, resulted in rapid formation of a water-soluble metabolite, identified as oestradiol 3-sulphate. 2. No evidence was obtained for the formation of other metabolic derivatives by… (More)
Several methylated derivatives of trilostane were prepared. Methylation of C-4 or C-4 and C-17 changes this relatively selective adrenal inhibitor to compounds with increased ovarian/placental inhibitory activity with decreased adrenal inhibitory activity.
Adenosine 3'5'-cyclic phosphate stimulated the conversion of added cholesterol to pregnenolone in "coupled" rat adrenal mitochondria provided with succinate, and in "leaky" mitochondria fortified with reduced nicotinamide adenine dinucleotide phosphate. Adenine nucleotides other than adenosine 3',5'-cyclic phosphate did not duplicate these actions. The… (More)
Azastene is an orally effective "luteolytic" agent in rhesus monkeys. In nonpregnant monkeys it reverses the human chorionic gonadotropin-stimulated increase in progesterone production and delay in the onset of menstruation, and, in inseminated monkeys, it prevents pregnancy if given for 5 days beginning on day 24 of the menstrual cycle. The drug is also… (More)