Ohnishi H, Ito C, Suzuki K, Niho T, Imaizumi Y, Yamazaki Y, Morishita S, Shimora M, Ito R
Nihon Yakurigaku Zasshi. 1980 Sep;76(6):469-77.
Effects of 5-methyl-7-diethylamino-s-triazolo-1, 5-a) pyrimidine (trapidil, Rocornal), a therapeutic agent for ischemic heart disease, on various types of experimental hyperlipemias were studied. With administration of trapidil, elevation of serum high density lipoprotein cholesterol (HDL-C) levels and reduction in serum total cholesterol (TC), low density lipoprotein and very low density lipoprotein cholesterol (LDL-C) and the ratio of HDL-C to LDL-C (LDL-C/HDL-c) were observed in most disease models. Changes in HDL-C levels and LDL-C/HDL-C in the hyperlipemia induced by lipid-enriched diet in mice and in the hyperlipemia induced by high cholesterol diet in Japanese quails were of statistical significance. Also, amelioration of reduction in HDL-C induced by high fat emulsion plus 6-n-propyl-2-thiouracil in rats was observed to be significant. Moreover, trapidil significantly reduced TC, LDL-C levels and LDL-C/HDL-C in the hyperlipemia in hamsters. To investigate possible mechanisms of therapeutic effects of trapidil, blood enzyme activities in Japanese quails with hyperlipemia were assayed. Trapidil showed increases in plasma lipoprotein lipase and serum lecithin-cholesterol acyltransferase activities. These results suggest that trapidil may be an effective chemotherapeutic agent for treating ischemic heart disease.
研究了用于治疗缺血性心脏病的药物5-甲基-7-二乙氨基-s-三唑并-1,5-a)嘧啶（曲匹地尔，乐可安）对各种类型实验性高脂血症的影响。给予曲匹地尔之后，在大多数疾病模型中观察到血清高密度脂蛋白胆固醇（HDL-C）水平升高，血清总胆固醇（TC）、低密度脂蛋白和极低密度脂蛋白胆固醇（LDL-C）降低，以及HDL-C与LDL-C的比值（LDL-C/HDL-c）降低。在小鼠高脂饮食诱导的高脂血症以及日本鹌鹑高胆固醇饮食诱导的高脂血症中，HDL-C水平和LDL-C/HDL-C的变化具有统计学意义。此外，观察到曲匹地尔对大鼠高脂肪乳剂加6-正丙基-2-硫氧嘧啶诱导的HDL-C降低有显著改善作用。此外，曲匹地尔显著降低了仓鼠高脂血症中的TC、LDL-C水平以及LDL-C/HDL-C。为了研究曲匹地尔治疗作用的可能机制，对患有高脂血症的日本鹌鹑的血液酶活性进行了测定。曲匹地尔使血浆脂蛋白脂肪酶和血清卵磷脂胆固醇酰基转移酶活性增加。这些结果表明，曲匹地尔可能是治疗缺血性心脏病的有效化疗药物。
