It is well known that adenosine is an important intermediary metabolite, acting as a building block for nucleic acids and a component of the biological energy currency ATP. In addition, adenosine functions as a signalling molecule through the activation of four distinct adenosine receptors — denoted A1, A2A, A2B and A3. These receptors are widely expressed and have been implicated in several biological functions, both physiological and pathological. These include cardiac rhythm and circulation, lipolysis, renal blood flow, immune function, sleep regulation and angiogenesis, as well as inflammatory diseases, ischaemia-reperfusion and neurodegenerative disorders.
The possibility of therapeutically targeting adenosine receptors is clear and has been so for a long time. Selective adenosine receptor agonists and antagonists are available and several trials are currently in progress. The greatest challenge in developing adenosine receptor ligands for specific clinical applications is that adenosine signalling is so widespread. Adenosine itself is present ubiquitously, adenosine receptors are widely distributed throughout the body. [1]
[1] Chen, J.-F., Eltzschig, H. K., & Fredholm, B. B. (2013). Adenosine receptors as drug targets — what are the challenges? Nature Reviews Drug Discovery, 12(4), 265–286. doi:10.1038/nrd3955
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