Inhibition of Cholesterol Biosynthesis in the Rat by 3 -(2-diethylaminoethoxy)androst-5-en-17-one, hydrochloride

Abstract

Summary 1. U-18666A, a new inhibitor of cholesterol biosynthesis, caused marked reduction in serum and liver sterols and appearance of desmosterol in livers of rats. 2. Reduction of serum sterols by U-18666A was obtained in animals in which hypercholesterolemia was induced with Triton WR-1339. 3. U-18666A increased incorporation of acetate-1-C¹⁴ into liver digitonin precipitable sterols fourfold and into liver fatty acids twofold. 4. Of several other compounds tested for cholesterol inhibitory activity, only hexestrol bis-β-diethylaminoethyl ether was found to cause appearance of desmosterol.