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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Chemistry, Physiology, and Pharmacology of β-Adrenergic Mechanisms in the Heart. Why are β-Blocker Antiarrhythmics Superior?

Author(s): A. Jozsef Szentmiklosi, Norbert Szentandrassy, Bence Hegyi, Balazs Horvath, Janos Magyar, Tamas Banyasz and Peter P. Nanasi

Volume 21, Issue 8, 2015

Page: [1030 - 1041] Pages: 12

DOI: 10.2174/1381612820666141029111240

Price: $65

Abstract

Stimulation of β-adrenergic receptors in the heart is the most effective endogenous way to increase the mechanical performance of cardiac tissues to meet the requirements of a fight-or-flight situation or stress. On the other hand, sustained activation of cardiac β-receptors initiates maladaptive remodeling of the myocardium leading to cardiomyopathies and heart failure. Since both acute and chronic stimulation of β-adrenoceptors are arrhythmogenic, the application of β-receptor blockers exerts effective antiarrhytmic actions at both short and long time scale. Compared to other classes of antiarrhythmic agents, β-blockers are the class of antiarrhythmics that was shown to decrease mortality in postinfarct patients. Chemical, physiological, and pharmacological properties of the β-adrenoceptor related signaling, the role of β-1, β-2, and β-3 receptor subtypes, consequences of acute and long term β-adrenergic stimulation and the underlying proarrhythmic mechanisms, including the changes in cardiac ion currents and Ca2+ handling, are reviewed in this paper together with the clinical relevance of cardioprotective β-blocking therapy.

Keywords: β-adrenergic receptors, β-receptor blockers, proarrhythmic mechanisms, antiarrhythmic drugs, cardiac ion currents, cardiac remodeling.


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