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Pathophysiological relevance of the cardiac β2-adrenergic receptor and its potential as a therapeutic target to improve cardiac function

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EUROPEAN JOURNAL OF PHARMACOLOGY
卷 698, 期 1-3, 页码 39-47

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ELSEVIER
DOI: 10.1016/j.ejphar.2012.11.001

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Beta-adrenoceptors; Cardiac contractility; Cardiac arrhythmias; Cardiac metabolism; Cardiac apoptosis

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beta-adrenoceptors are members of the G protein-coupled receptor superfamily which play a key role in the regulation of myocardial function. Their activation increases cardiac performance but can also induce deleterious effects such as cardiac arrhythmias or myocardial apoptosis. In fact, inhibition of beta-adrenoceptors exerts a protective effect in patients with sympathetic over-stimulation during heart failure. Although beta(2)-adrenoceptor is not the predominant subtype in the heart, it seems to importantly contribute to the cardiac effects of adrenergic stimulation; however, the mechanism by which this occurs is not fully understood. This review summarizes the current knowledge on the role of beta(2)-adrenoceptors in the regulation of cardiac contractility, metabolism, cardiomyocyte survival and cardiac arrhythmias. In addition, therapeutic considerations relating to stimulation of the beta(2)-adrenoceptor such as an increase in cardiac contractility with low arrythmogenic effect, protection of the myocardium again apoptosis or positive regulation of heart metabolism are discussed. (C) 2012 Elsevier B.V. All rights reserved.

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