Dissociating the effects of A2A agonism

The vasodilatory effects of adenosine A2A receptor agonists make them useful as cardiac stress agents in imaging but have made it difficult to exploit these molecules' potent anti-inflammatory effects.¹ Researchers in Germany have dissociated the anti-inflammatory effects of adenosine A_2A receptor agonists from their hemodynamic effects and are determining a specific inflammation-related indication to pursue with the molecule.²

Activation of the adenosine A_2A receptor (ADORA2A) on endothelial cells promotes vasodilation, and activation of the receptor on immune cells inhibits inflammatory processes. The vasodilatory effects become dose-limiting side effects in the inflammation setting by causing hypotension, which in turn triggers a compensatory increase in heart rate and cardiac output...