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