Abstract.

Activation of the adenosine A_2A receptor by adenosine or synthetic agonists is regarded as a promising approach in the treatment of allergic pulmonary diseases and diabetic ulcers, in the prevention of ischemia-reperfusion injury, in the diagnostics of cardiac ischemia. Agonists of A_2AARs have been clinically evaluated for different medical indications, but a limited success has been achieved, because of the side effects, short half-life and a lack of effect in some cases. At present, only adenosine and regadenosone are marketed as diagnostic tools in the USA and Europe. It is evident that there is a necessity of searching for new agonists with improved affinity and selectivity profiles, which is mainly achieved by modifying the existing ligands.

The purpose of this review is to discuss in brief the structure-activity relationships of A_2AAR agonists in light of the known crystallographic data about the receptor. The main therapeutic applications of the A_2AAR agonists are also reviewed.