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首页> 外文期刊>Life sciences >Different changes of plasma membrane beta-adrenoceptors in rat heart after chronic administration of propranolol, atenolol and bevantolol
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Different changes of plasma membrane beta-adrenoceptors in rat heart after chronic administration of propranolol, atenolol and bevantolol

机译：长期服用普萘洛尔，阿替洛尔和倍他洛尔后大鼠心脏质膜β-肾上腺素受体的不同变化

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Recently, tissue segment binding method with a hydrophilic radioligand [H-3]-CGP12177 was developed to detect plasma membrane beta-adrenoceptors in rat heart (Horinouchi et al., 2006). In the present study, propranolol (40 mg kg(-1) day(-1)), atenolol (40 mg kg-(1) day(-1)) and bevantolol (200 mg kg(-1) day(-1)) were administered to rats for 6 weeks, and the changes of plasma membrane beta-adrenoceptors and their mRNA expression in rat ventricle were examined. Chronic administration of propranolol increased the beta(1)-adrenoceptors but decreased the beta(2)-adrenoceptors without changing total amount of plasma membrane beta-adrenoceptors. Atenolol increased both plasma membrane beta(1)- and beta(2)-adrenoceptors, whereas bevantolol had no effect on the beta-adrenoceptor density and their subtype proportions. In contrast, the density of beta-adrenoceptors detected in conventional homogenate binding study was extremely low (approximately 60% of plasma membrane beta-adrenoceptors detected with the tissue segment binding method) and the effects of chronic administration of p-adrenoceptor antagonists were not necessarily in accord with those at the plasma membrane beta-adrenoceptors. The mRNA levels of beta(1)- and beta(2)-adrenoceptors were not altered by propranolol treatment, while beta(1)-adrenoceptor mRNA significantly decreased after administration of atenolol or bevantolol without changing the level of beta(2)-adrenoceptor mRNA. The present binding study with intact tissue segments clearly shows that the plasma membrane beta(1)- and beta(2)-adrenoceptors of rat heart, in contrast to the homogenate binding sites and the mRNA levels, are differently affected by chronic treatment with three beta-adrenoceptor antagonists; up- and down-regulations of beta(1)- and beta(2)-adrenoceptors, respectively, by propranolol, and up-regulation of both the subtypes by atenotol, but no significant change in both the subtypes by bevantolol. (c) 2007 Elsevier Inc. All rights reserved.
机译：最近，开发了一种使用亲水性放射性配体[H-3] -CGP12177的组织片段结合方法来检测大鼠心脏的质膜β-肾上腺素能受体（Horinouchi等，2006）。在本研究中，普萘洛尔（40 mg kg（-1）天（-1）），阿替洛尔（40 mg kg-（1）天（-1））和贝伐洛尔（200 mg kg（-1）天（-1） ））给予大鼠6周，检查大鼠心室中质膜β-肾上腺素受体的变化及其mRNA表达。长期服用普萘洛尔可增加β（1）-肾上腺素受体，但减少β（2）-肾上腺素受体，而不会改变质膜β-肾上腺素受体的总量。阿替洛尔增加了质膜β（1）-和β（2）-肾上腺素受体，而贝伐洛尔对β-肾上腺素受体密度及其亚型比例没有影响。相比之下，在常规匀浆结合研究中检测到的β-肾上腺素受体的密度极低（约60％的组织膜结合法检测到的质膜β-肾上腺素受体），而长期服用p-肾上腺素受体拮抗剂的效果并不一定与质膜β-肾上腺素能受体一致。普萘洛尔治疗不会改变β（1）-和β（2）-肾上腺素受体的mRNA水平，而在服用阿替洛尔或贝伐洛尔后，β（1）-肾上腺素受体mRNA显着下降，而不会改变β（2）-肾上腺素受体的水平mRNA。目前对完整组织片段的结合研究清楚地表明，与匀浆结合位点和mRNA水平相比，大鼠心脏的质膜β（1）-和β（2）-肾上腺素能受体受到慢性治疗的不同影响，三种β-肾上腺素受体拮抗剂;普萘洛尔分别分别上调和下调β（1）-和β（2）-肾上腺素受体，而阿替诺尔分别上调两种亚型，但贝伐洛尔对两种亚型均无显着变化。 （c）2007 Elsevier Inc.保留所有权利。

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