Updates in the function and regulation of α1‐adrenoceptors

Juliana Akinaga; André S. Pupo

doi:10.1111/bph.14617

journal article Apr 01, 2019

Updates in the function and regulation of α1‐adrenoceptors

Juliana Akinaga

André S. Pupo

British Journal of Pharmacology Vol. 176 No. 14 pp. 2343-2357 · Wiley

View at Publisher Save 10.1111/bph.14617

Abstract

α1‐Adrenoceptors are seven transmembrane domain GPCRs involved in numerous physiological functions controlled by the endogenous catecholamines, noradrenaline and adrenaline, and targeted by drugs useful in therapeutics. Three separate genes, whose products are named α1A‐, α1B‐, and α1D‐ adrenoceptors, encode these receptors. Although the existence of multiple α1‐adrenoceptors has been acknowledged for almost 25 years, the specific functions regulated by each subtype are still largely unknown. Despite the limited comprehension, the identification of a single class of subtype‐selective ligands for the α1A‐ adrenoceptors, the so‐called α‐blockers for prostate dysfunction, has led to major improvement in therapeutics, demonstrating the need for continued efforts in the field. This review article surveys the tissue distribution of the three α1‐adrenoceptor subtypes in the cardiovascular system, genitourinary system, and CNS, highlighting the functions already identified as mediated by the predominant activation of specific subtypes. In addition, this review covers the recent advances in the understanding of the molecular mechanisms involved in the regulation of each of the α1‐adrenoceptor subtypes by phosphorylation and interaction with proteins involved in their desensitization and internalization.Linked ArticlesThis article is part of a themed section on Adrenoceptors—New Roles for Old Players. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.14/issuetoc

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Details

Published: Apr 01, 2019
Vol/Issue: 176(14)
Pages: 2343-2357
License: View

Authors

J

Juliana Akinaga

Department of Pharmacology Instituto de Biociências, UNESP Botucatu Brazil

A

André S. Pupo

Department of Pharmacology Instituto de Biociências, UNESP Botucatu Brazil

Funding

Consejo Nacional de Ciencia y Tecnología Award: 253156

Cite This Article

Juliana Akinaga, André S. Pupo (2019). Updates in the function and regulation of α1‐adrenoceptors. British Journal of Pharmacology, 176(14), 2343-2357. https://doi.org/10.1111/bph.14617

Updates in the function and regulation of α1‐adrenoceptors

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