Recent Advances in the Discovery of 1-Adrenoceptor Agonists

Publisher: Bentham Science Publishers

E-ISSN: 1873-4294|7|2|135-145

ISSN: 1568-0266

Source: Current Topics in Medicinal Chemistry, Vol.7, Iss.2, 2007-01, pp. : 135-145

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Abstract

The 1 adrenoceptors are three of nine well-characterized receptors that are activated by epinephrine and norepinephrine. Agonists acting at the 1 adrenoceptors produce numerous physiological effects, and are used therapeutically for several indications. Many known 1 adrenoceptor agonists are 1A selective, but the discovery of highly selective 1B and 1D 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 1 agonists as well as contributions to our understanding of agonist-receptor interactions.