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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Agonists and Antagonists Targeting the Different α2-Adrenoceptor Subtypes

Author(s): Francesco Gentili, Maria Pigini, Alessandro Piergentili and Mario Giannella

Volume 7, Issue 2, 2007

Page: [163 - 186] Pages: 24

DOI: 10.2174/156802607779318235

Price: $65

Abstract

Chemical and biological strategies have provided evidence for α2-receptor heterogeneity, to date classified in three different subtypes, α2A, α2B, and α2C. These are widely distributed throughout the body and mediate numerous effects; therefore, the potential therapeutic indications of agonists and antagonists are numerous. Nevertheless, the lack of subtype-selectivity of the well-known compounds represents a major limit for their use. SAR studies may help to design new and more selective drugs.

Keywords: α2-adrenoceptor agonists, α2-adrenoceptor antagonists, α2-adrenoceptor subtypes, therapeutic uses of α2-ligands, imidazoline binding sites, α2-adrenoceptor subtypes-mediated effects


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