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新型降脂化合物盐酸乙噻酯的动物实验研究(作者译)

[Expeimental studies in animals on a new lipid lowering compound: etiroxate hydrochloride (author's transl)].

作者信息

Beckmann R

出版信息

Arzneimittelforschung. 1979;29(3):499-508.

PMID:582735
Abstract

D,L-alpha-Methyl-thyroxin-ethylester hydrochloride (etiroxate hydrochloride, CG 635, Skleronorm) has been proved to be highly effective in lowering serum lipids in rats. Even daily oral doses of 3.3 mumol etiroxate hydrochloride/kg (2.8 mg/kg) decrease serum cholesterol significantly in hypercholesterolemic rats. From a dose of 10 mg/kg upwards etiroxate hydrochloride also significantly reduces serum triglycerides. Etiroxate hydrochloride has much less effect on oxygen consumption, heart rate and heart weight of rats than have L-thyroxin and D-thyroxin, and its antigoitrogenic effect is also much slighter. As calculated from the ratio between relative effect on basal metabolism and relative effect on serum cholesterol, the relative therapeutic index of the compound is 10--35 in comparison to a relative therapeutic index of 1 for L-thyroxin and D-thyroxin.

摘要

盐酸D,L-α-甲基甲状腺素乙酯(盐酸乙碘 thyroxate,CG 635,Skleronorm)已被证明对降低大鼠血清脂质非常有效。即使每天口服3.3 μmol盐酸乙碘 thyroxate/千克(2.8毫克/千克),也能显著降低高胆固醇血症大鼠的血清胆固醇。从10毫克/千克起,盐酸乙碘 thyroxate也能显著降低血清甘油三酯。盐酸乙碘 thyroxate对大鼠的耗氧量、心率和心脏重量的影响比L-甲状腺素和D-甲状腺素小得多,其抗甲状腺肿作用也轻得多。根据对基础代谢的相对作用与对血清胆固醇的相对作用之比计算,该化合物的相对治疗指数为10-35,而L-甲状腺素和D-甲状腺素的相对治疗指数为1。

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