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
Current Topics in Medicinal Chemistry
Title: Agonists and Antagonists Targeting the Different α2-Adrenoceptor Subtypes
Volume: 7 Issue: 2
Author(s): Francesco Gentili, Maria Pigini, Alessandro Piergentili and Mario Giannella
Affiliation:
Keywords: α2-adrenoceptor agonists, α2-adrenoceptor antagonists, α2-adrenoceptor subtypes, therapeutic uses of α2-ligands, imidazoline binding sites, α2-adrenoceptor subtypes-mediated effects
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.
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Cite this article as:
Gentili Francesco, Pigini Maria, Piergentili Alessandro and Giannella Mario, Agonists and Antagonists Targeting the Different α2-Adrenoceptor Subtypes, Current Topics in Medicinal Chemistry 2007; 7 (2) . https://dx.doi.org/10.2174/156802607779318235
DOI https://dx.doi.org/10.2174/156802607779318235 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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