Nilutamide is a non-steroidalandrogen receptor antagonist and also inhibits androgen biosynthesis in vitro.
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Nilutamide (Nilandron) is an orally active, nonsteroidal androgen receptor antagonist that binds to androgen receptors without affinity for progestogen, estrogen, or glucocorticoid receptors. Nilutamide is used in prostate cancer research and possesses antischistosomal properties[1][4].
体内研究
Nilutamide (50-400 mg/kg; pO.; single dosage) decreases the worm burdens of juvenile and adult Schistosoma mansoni cercariae in infected mice [4].
体外研究
Nilutamide (110 μM) inhibits several enzyme activities in human liver microsomes: hexobarbital hydroxylase by 85%, benzphetamine N-demethylase by 40%, benzo(a)pyrene hydroxylase by 35%, and 7-ethoxycoumarin O-deethylase by 25%[2].
Nilutamide (550 μM) exhibits no significant impact on NADPH consumption by aerobic microsomes, nor does it alter the kinetics of cytochrome P-450 reduction by NADPH-cytochrome P-450 reductase in an anaerobic environment [2].
Nilutamide inhibits the significant elevation of GCDFP-15 release triggered by 1 nM testosterone in T-47D cells and ZR-75-1 cells, with IC50 values of 87 nM and 75 nM, respectively [3].
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