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Trends Pharmacol Sci. 2006 Jun;27(6):330-7. Epub 2006 May 11.

Subtype-specific alpha1- and beta-adrenoceptor signaling in the heart.

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  • 1Institute of Molecular Medicine, Peking University, Beijing 100871, China.


Recent studies of adrenoceptors have revealed subtype-specific signaling, promiscuous G-protein coupling, time-dependent switching of intracellular signaling pathways, intermolecular interactions within or between adrenoceptor subfamilies, and G-protein-independent signaling pathways. These findings have extended the classical linear paradigm of G-protein-coupled receptor signaling to a complex "signalome" in which an individual adrenoceptor initiates multiple signaling pathways in a temporally and spatially regulated manner. In particular, persistent stimulation of beta-adrenoceptor subtypes causes a time-dependent switch of signaling pathways and elicits different, even opposing, functional roles of these receptors in regulating cardiac structure and function. Recent progress in the understanding of subtype-specific functions and signaling mechanisms of cardiac adrenoceptor subtypes, particularly beta(1)-adrenoceptors, beta(2)-adrenoceptors, alpha(1A)-adrenoceptors and alpha(1B)-adrenoceptors, might have important pathogenic and therapeutic implications for heart disease.

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