Agonists and Antagonists Targeting the Different α2-Adrenoceptor Subtypes

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.

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