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6-氯-9-[2-(6-甲基-3-吡啶基)乙基]-1,2,3,4-四氢咔唑-2-羧酸的血清降脂特性

Serum lipid-lowering properties of 6-chloro-9-[2-(6-methyl-3-pyridyl)ethyl]-1,2,3,4-tetrahydrocarbazole-2-carboxylic acid.

作者信息

Dalton C, Pool W R

出版信息

J Pharm Sci. 1977 Mar;66(3):348-52. doi: 10.1002/jps.2600660311.

Abstract

6-Chloro-9-[2-(6-methyl-3-pyridyl)ethyl]-1,2,3,4-tetrahydrocarbazole-2-carboxylic acid hydrochloride lowered serum cholesterol, triglyceride, phospholipid, and free fatty acid levels in normal rats. The compound appeared to have a low toxicity and to be well tolerated in mice, adult and neonatal rats, and rabbits. At hypolipidemic doses, it caused a slight hepatomegaly associated with an increase in liver phospholipid and protein content. Liver N-demethylase and catalase activities were increased by the drug treatment. This acid had no in vitro antilipolytic activity and did not affect serum desmosterol-cholesterol ratios. The results indicate that it has a mechanism of action similar to clofibrate.

摘要

6-氯-9-[2-(6-甲基-3-吡啶基)乙基]-1,2,3,4-四氢咔唑-2-羧酸盐酸盐可降低正常大鼠的血清胆固醇、甘油三酯、磷脂和游离脂肪酸水平。该化合物似乎毒性较低,在小鼠、成年和新生大鼠以及兔子中耐受性良好。在降血脂剂量下,它会引起轻微肝肿大,并伴有肝脏磷脂和蛋白质含量增加。药物治疗可提高肝脏N-脱甲基酶和过氧化氢酶的活性。这种酸在体外没有抗脂解活性,也不影响血清胆甾烷醇-胆固醇比率。结果表明其作用机制与氯贝丁酯相似。

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