Adrian R W, Ismail S, Jahn U
Arzneimittelforschung. 1983;33(10):1464-8.
A new diphenylmethane derivative with potent hypolipidemic activity, ethyl-(+/-)-2-[[alpha-(p-chlorophenyl)-p-tolyl]-oxy]-2-methylbutyrate (Sgd 24774, beclobrate) has been investigated in animals. From a comparison of the ED25 values of beclobrate and clofibrate, the new drug is 11 times more potent with respect to its hypocholesterolemic activity and 36 times more hypotriglyceridemic in normally fed rats, and lowers fructose-induced hypertriglyceridemia in rats 20 times as effectively as does clofibrate. On a similar basis of comparison, the hepatomegalic effect of beclobrate in rats is 22 times that of clofibrate. High doses of beclobrate did not reveal any other peripheral or central effects in a wide range of pharmacological tests, indicating a high specificity of the action of the drug on blood lipids. On the basis of the results of interaction studies performed with beclobrate in animals, administration of the substance in man should be largely free from risk.
一种具有强效降血脂活性的新型二苯甲烷衍生物,乙基-(+/-)-2-[[α-(对氯苯基)-对甲苯基]氧基]-2-甲基丁酸酯(Sgd 24774,氯贝酸铝)已在动物身上进行了研究。通过比较氯贝酸铝和氯贝丁酯的ED25值,在正常喂养的大鼠中,这种新药的降胆固醇活性高11倍,降甘油三酯活性高36倍,降低果糖诱导的大鼠高甘油三酯血症的效果是氯贝丁酯的20倍。在类似的比较基础上,氯贝酸铝对大鼠肝脏肿大的影响是氯贝丁酯的22倍。在广泛的药理学试验中,高剂量的氯贝酸铝未显示出任何其他外周或中枢作用,表明该药物对血脂的作用具有高度特异性。根据在动物身上用氯贝酸铝进行的相互作用研究结果,在人体中使用该物质应基本无风险。