Recent studies indicate a widening role for adenosine receptors in many therapeutic areas. Adenosine receptors are involved in immunological and inflammatory responses, respiratory regulation, the cardiovascular system, the kidney, various CNS-mediated events including sleep and neuroprotection, as well as central and peripheral pain processes. In this review, the physiological role of adenosine receptors in these key areas is described with reference to the therapeutic potential of adenosine receptor agonists and antagonists.