Recent progress in α1-adrenoceptor pharmacology

Abstract

The adrenoceptors (ARs) play a key role in the modulation of sympathetic nervous system activity and are a site of action for many clinically important therapeutic agents. The α1-adrenoceptor subtypes (α1A-, α1B-, and α1D-AR) play a prominent role in regulating vascular tone and hypertrophic growth of smooth muscle and cardiac cells. Their functional characteristics with respect to ligand binding and second messenger utilization have been well described. Here, we review recent progress on subtype-specific subcellular localization, participation in signaling cascades, and the pivotal function of α1-ARs, as delineated through studies on genetically engineered animals. Together, these findings will provide new insights into the physiological and pathophysiological roles of the α1-ARs.