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6-氨基-2-巯基-5-甲基嘧啶-4-羧酸及相关衍生物在啮齿动物中的降血脂活性

Hypolipidemic activity of 6-amino-2-mercapto-5-methyl-pyrimidine-4-carboxylic acid and related derivatives in rodents.

作者信息

Hall I H, Cocolas G H, Murthy A R, Rhyne K A, Knowles M

出版信息

J Pharm Sci. 1985 Jul;74(7):759-64. doi: 10.1002/jps.2600740713.

Abstract

6-Amino-2-mercapto-5-methylpyrimidine-4-carboxylic acid proved to be a potent hypolipidemic agent in rodents at the low dose of 20 mg/kg/d. The agent effectively reduced the liver enzyme activities required for the synthesis of triglycerides and cholesterol. Lower lipid levels in tissue were observed in mice but not in rats. Preliminary studies indicate that the agent accelerated the excretion of cholesterol and its metabolites from the body. The agents lowered the low-density lipoprotein (LDL) cholesterol content and raised the high-density lipoprotein (HDL) cholesterol content. These changes in lipoprotein cholesterol content suggest that the agent may be helpful in protecting against coronary disease. The agent is more effective than the commercially available agent, i.e., clofibrate at 150 mg/kg/d.

摘要

6-氨基-2-巯基-5-甲基嘧啶-4-羧酸在20毫克/千克/天的低剂量下被证明是一种有效的降血脂剂,对啮齿动物有效。该药剂有效降低了甘油三酯和胆固醇合成所需的肝脏酶活性。在小鼠中观察到组织中的脂质水平降低,但在大鼠中未观察到。初步研究表明,该药剂加速了胆固醇及其代谢产物从体内的排泄。该药剂降低了低密度脂蛋白(LDL)胆固醇含量,提高了高密度脂蛋白(HDL)胆固醇含量。脂蛋白胆固醇含量的这些变化表明该药剂可能有助于预防冠心病。该药剂比市售药剂氯贝丁酯(150毫克/千克/天)更有效。

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