Jpn. J. Pharmacol. 86 (1), 120-123 (2001)

NTE-122, an Acyl-CoA:Cholesterol Acyltransferase Inhibitor, Prevents the Progression of Atherogenesis in Cholesterol-Fed Rabbits

Yukimasa Azuma*, Katsuhiro Date, Katsutoshi Ohno, Shoichiro Matsushiro, Yoichi Nobuhara and Toshihiro Yamada

Central Research Institute, Nissin Food Products Co., Ltd., 2247, Noji, Kusatsu, Shiga 525-0055, Japan

*Corresponding author. FAX: +81-77-561-9108, E-mail:

Abstract: The cholesterol-lowering and anti-atherosclerotic effects of NTE-122 (trans-1,4-bis[[1-cyclohexyl-3-(4-dimethylaminophenyl)ureido]methyl]cyclohexane), an acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, were evaluated in 1% cholesterol diet-fed rabbits. NTE-122 (1, 3 and 10 mg/kg per day) lowered the total cholesterol levels in both plasma and liver dose-dependently (by 99% and 94% at 10 mg/kg per day, respectively). In the aortic wall of the rabbits given NTE-122, the atherosclerotic lesion area in both aortic arch and thoracic aorta were dose-dependently reduced (by 100% at 10 mg/kg per day), and the total cholesterol content in aortic arch was also lowered significantly at more than 3 mg/kg per day. These results suggest that NTE-122 is capable of exhibiting anti-atherosclerotic effects.

Keywords: NTE-122, Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, Atherosclerosis
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