CGS 21680 is a potent, selective agonist of the adenosine A2A receptor (Ki = 11-46 nM). It is less effective at adenosine A1 and A3 receptors (Kis = 0.5-3.1 and 0.6-1 μM, respectively) and is without effect at adenosine A2B (Ki > 10 μM). CGS 21680 is commonly used to study the actions of the adenosine A2A receptor in cells and tissues.