U-73482: A novel ACAT inhibitor that elevates HDL-cholesterol, lowers plasma triglyceride and facilitates hepatic cholesterol mobilization in the rat

摘要: U-73482, a novel acylCoA:cholesterol acyltransferase (ACAT) inhibitor with systemic activity, has been evaluated for its effects on variety of lipid metabolic parameters in the rat. The compound inhibits ACAT vitro cultured Fu5AH rat hepatoma cells and demonstrates activity through inhibition hepatic rats receiving drug orally. U-73482 also lowers plasma triglycerides at 40 mg/kg per day elevates high density lipoprotein cholesterol (HDL-chol) dose-related fashion over range daily intakes 0-40 Elevations HDL-chol are followed by elevations total normal but exerts hypocholesterolemic cholesterol-fed promotes clearance stored sterol pretreated hypercholesterolemic diet then changed to chow. triglyceride-lowering elevating coupled ability promote tissue block dietary animals, suggests that potential as therapeutic agent treatment disorders man.