Kritchevsky D, Tepper S A, Mueller M A, Klurfeld D M
Arzneimittelforschung. 1983;33(10):1469-71.
Two new hypocholesterolemic compounds, ethyl-(+/-)-2-[[alpha-(p-chlorophenyl)-p-tolyl]-oxy]-2-methylbutyrate (Sgd 24 774, beclobrate) and the 3-pyridinylmethyl ester (eniclobrate), have been studied in normocholesterolemic rats. The two compounds are hepatomegalic and they lower serum and liver cholesterol levels but raise liver triglyceride levels. They also reduce the percentage of esterified cholesterol present in the serum. Beclobrate enhances hepatic HMG-CoA reductase activity but does not affect cholesterol-7 alpha hydroxylase. Eniclobrate, on the other hand, increases activity of the hydroxylase but not of HMG-CoA reductase. Neither compound affects cholesterol absorption.
两种新型降胆固醇化合物,乙基-(±)-2-[[α-(对氯苯基)-对甲苯基]氧基]-2-甲基丁酸酯(Sgd 24 774,贝氯贝特)和3-吡啶基甲酯(烯氯贝特),已在正常胆固醇水平的大鼠中进行了研究。这两种化合物会导致肝脏肿大,它们能降低血清和肝脏中的胆固醇水平,但会提高肝脏中的甘油三酯水平。它们还会降低血清中酯化胆固醇的百分比。贝氯贝特可增强肝脏HMG-CoA还原酶活性,但不影响胆固醇7α羟化酶。另一方面,烯氯贝特可提高羟化酶的活性,但不提高HMG-CoA还原酶的活性。这两种化合物均不影响胆固醇的吸收。