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抗血脂药物。第2部分:一种新型强效抗血脂药物异丙基-[4'-(对氯苯甲酰基)-2-苯氧基-2-甲基]-丙酸酯(LF178)的实验研究。

Antilipidemic drugs. Part 2: Experimental study of a new potent hypolipidemic drug, isopropyl-[4'-(p-chlorobenzoyl)-2-phenoxy-2-methyl]-propionate (LF178).

作者信息

Gurrieri J, Lous M L, Renson F J, Tourne C, Voegelin H, Majoie B, Wüfert E

出版信息

Arzneimittelforschung. 1976;26(5):889-94.

PMID:989363
Abstract

Pharmacological investigations have been carried out on a new p-chlorobenzoyl substituted phenoxy-isobutyric acid derivate with potent antilipidemic activity, isopropyl-[4'-(p-chlorobenzoyl)-2-phenoxy-2-methyl]propionate (LF 178; procetofene; Lipanthyl¿). The compound depressed total lipids and total cholesterol significantly in the normal rat from 15-20 mg/kg upwards. At 100 mg/kg, the drug-induced depression of total lipids was twice the effect observed with 300 mg/kg of clofibrate. Significant depression of lipid parameters was induced in the senescent rat, in the dietary hyperlipidemic and in the triton hyperlipidemic rat. In the two last models clofibrate failed to affect lipid parameters at 300 mg/kg. The absence of pharmacological side effects indicates a high pharmacological specificity with respect to lipid metabolism. It might be concluded that LF 178 presents an antilipidemic profile different from the well known hypolipidemic drug clofibrate.

摘要

已对一种具有强效降血脂活性的新型对氯苯甲酰基取代苯氧基异丁酸衍生物异丙基-[4'-(对氯苯甲酰基)-2-苯氧基-2-甲基]丙酸酯(LF 178;普罗布考;利平脂®)进行了药理学研究。该化合物在正常大鼠中,从15 - 20毫克/千克及以上剂量时能显著降低总脂质和总胆固醇。在100毫克/千克剂量时,药物引起的总脂质降低效果是300毫克/千克氯贝丁酯所观察到效果的两倍。在衰老大鼠、饮食性高脂血症大鼠和 Triton 高脂血症大鼠中均诱导出脂质参数的显著降低。在最后两种模型中,300毫克/千克的氯贝丁酯未能影响脂质参数。无药理副作用表明对脂质代谢具有高度的药理学特异性。可以得出结论,LF 178呈现出与著名的降血脂药物氯贝丁酯不同的降血脂谱。

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