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β-肾上腺素能受体阻滞剂卡替洛尔和普萘洛尔对自发性高血压大鼠心脏肥大的剂量相关抑制作用。

Dose-related inhibitory effects of the beta-adrenoceptor blocking drugs carteolol and propranolol on cardiac hypertrophy in spontaneously hypertensive rats.

作者信息

Igawa T, Ikezono K, Watanabe K, Kimura Y

出版信息

Eur J Pharmacol. 1984 Sep 3;104(1-2):93-9. doi: 10.1016/0014-2999(84)90373-x.

Abstract

The inhibitory effect of two kinds of beta-adrenoceptor blocking drugs [propranolol: 1-100 mg/kg per day; carteolol: 0.3-30 mg/kg per day] on the development of cardiac hypertrophy was studied in young spontaneously hypertensive rats (SHR: 4 weeks old). Though neither propranolol or carteolol given for 6 weeks reduced the development of hypertension in SHR, both drugs did reduce the increase in the heart weight/body weight ratio in a dose-dependent manner. This potency of carteolol was about 300 times greater than that of propranolol. The potency of carteolol with regard to the reduction in the myocardial protein/DNA ratio was about 300 times greater than that of propranolol. The beta-blocking potency, estimated from the area under the dose-response curve (beta-blocking action) of carteolol, was also 300 times greater than that of propranolol and correlated well with the extent of the structural changes in the heart. Thus, the possibility that the degree of beta-blocking potency may strongly relate to structural changes in the heart of young SHR has to be given consideration.

摘要

在年轻的自发性高血压大鼠(SHR:4周龄)中,研究了两种β-肾上腺素能受体阻断药物[普萘洛尔:每天1-100mg/kg;卡替洛尔:每天0.3-30mg/kg]对心脏肥大发展的抑制作用。虽然给予普萘洛尔或卡替洛尔6周均未降低SHR的高血压发展,但两种药物均以剂量依赖性方式降低了心脏重量/体重比的增加。卡替洛尔的这种效力比普萘洛尔大300倍左右。卡替洛尔在降低心肌蛋白/DNA比值方面的效力比普萘洛尔大300倍左右。根据卡替洛尔的剂量-反应曲线下面积(β-阻断作用)估计的β-阻断效力也比普萘洛尔大300倍,并且与心脏结构变化的程度密切相关。因此,必须考虑β-阻断效力程度可能与年轻SHR心脏结构变化密切相关的可能性。

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