Recent Advances in the Discovery of α1-Adrenoceptor Agonists

The α1 adrenoceptors are three of nine well-characterized receptors that are activated by epinephrine and norepinephrine. Agonists acting at the α1 adrenoceptors produce numerous physiological effects, and are used therapeutically for several indications. Many known α1 adrenoceptor agonists are α1A selective, but the discovery of highly selective α1B and α1D adrenoceptor agonists has proven to be an extremely difficult goal to achieve. This review will focus on recent advances in the discovery, development and clinical utility of subtype-specific α1 agonists as well as contributions to our understanding of agonist-receptor interactions.