Liarozole dihydrochloride (R75251; R85246) 是一种细胞色素 P450 (CYP450) 依赖性抑制剂，具有口服活性，也是雌激素 (estrogen) 和睾丸雄激素合成的有效抑制剂。Liarozole dihydrochloride 通过抑制 4-羟化酶 (4-hydroxylase) 来防止视黄酸的分解代谢，并在体内显示出类视黄醇保留和类视黄醇模拟作用。Liarozole dihydrochloride 是咪唑衍生物; 它被作为前列腺癌和和皮肤病的非激素药物进行研究。
Liarozole inhibits the metabolism of retinoic acid to more polar metabolites in hamster liver microsomes (IC
50
=2.2 μM), rat liver homogenate (IC
50
=0.14 μM), dunning prostate cancer homogenate (IC
50
=0.26 μM) and MCF-7 human breast cancer cells (almost complete block at 10μM) .
Liarozole inhibits 17a-hydroxylase activity in bovine adrenal microsomes (IC
50
=0.15 μM) .
Liarozole has modest inhibitory activity on cholesterol synthesis in human hepatoma cells(IC
50
=5 μM).
