D, L-α-Methyl Thyroxine Ethyl Ester (CG-635)の脂質低下作用と基礎代謝, 心臓, 甲状腺への影響

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CG-635,a new thyroxine analog, was examined for its lipid-lowering effect and influence on basal metabolic rate (BMR), heart and thyroid gland in comparison with L-thyroxine (LT_4) and D-thyroxine (DT_4) . With daily doses of 3-30 mg/kg, CG-635 markedly reduced plasma cholesterol level in rats and rabbits fed a high cholesterol diet. The potency of these compounds in cholesterol-lowering activity was as follows : LT_4=DT_4> CG-635> clofibrate. In normal rats, CG-635 with a daily dose of 100 mg/kg showed no effect on BMR, heart rate, heart weight and thyroid gland weight, though LT_4 showed considerable effect even with the daily dose of 1.0 mg/kg. The effect of CG-635 on BMR, heart rate and heart weight in thiouracil- or methimazole-treated rats was 700 -3500 times less than that of LT_4,and 200-275 times less than that of DT_4. The relative activity of CG-635,DT_4 and LT_4 on BMR, heart rate and heart weight compared at the dose showing the same cholesterol-lowering potency was 1 : 4 : 12-60. These results suggested that CG-635 had a marked cholesterol-lowering activity without corresponding effect on BMR, heart and thyroid gland.
公益社団法人日本薬学会の論文
1974-12-25