Recent Progress in α1-Adrenoceptor Pharmacology

Taka-aki Koshimizu; Junji Yamauchi; Akira Hirasawa; Akito Tanoue; Gozoh Tsujimoto

doi:10.1248/bpb.25.401

Review

Recent Progress in α₁-Adrenoceptor Pharmacology

Taka-aki Koshimizu, Junji Yamauchi, Akira Hirasawa, Akito Tanoue, Gozoh Tsujimoto

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Keywords: α₁-adrenoceptor, cellular signaling, cellular localization, transgenic mouse, knockout mouse, pharmacogenomics

JOURNAL FREE ACCESS

2002 Volume 25 Issue 4 Pages 401-408

DOI https://doi.org/10.1248/bpb.25.401

Details

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 (α_1A-, α_1B-, and α_1D-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.

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