Agonists and antagonists targeting the different alpha2-adrenoceptor subtypes.
Chemical and biological strategies have provided evidence for alpha(2)-receptor heterogeneity, to date classified in three different subtypes, alpha(2A), alpha(2B), and alpha(2C). 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.
Gentili
Francesco
F
Department of Chemical Sciences, University of Camerino, via S. Agostino 1, 62032 Camerino, Italy.
Pigini
Maria
M
Piergentili
Alessandro
A
Giannella
Mario
M
D058647:Adrenergic alpha-2 Receptor Agonists; D058669:Adrenergic alpha-2 Receptor Antagonists; D000316:Adrenergic alpha-Agonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000317:Adrenergic alpha-Antagonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D006801:Humans; D018341:Receptors, Adrenergic, alpha-2 / Q000145:classification / Q000378:metabolism; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D058647:Adrenergic alpha-2 Receptor Agonists; D058669:Adrenergic alpha-2 Receptor Antagonists; D000316:Adrenergic alpha-Agonists; D000317:Adrenergic alpha-Antagonists; D018341:Receptors, Adrenergic, alpha-2