A3-adenosine receptors: Design of selective ligands and therapeutic prospects

Abstract

The A3 receptor has been established as a distinct receptor subtype through cloning and the synthesis of selective agonists. The distribution of this subtype in the body is unique and more limited than for A1 or A2 receptors. Actions associated with this subtype include mast cell degranulation, cerebroprotection, cardioprotection, and possibly alteration of fertility. The effects on the inflammatory system and the high level of A3 receptor expression in the lungs suggests the use of A3 antagonists for asthma. Thus, there is a tremendous potential for development for therapeutic purposes of selective drugs, either agonists or antagonists, acting at this receptor.