Identification of the A2 Adenosine Receptor Binding Subunit by Photoaffinity Crosslinking
Adenylate cyclase coupled adenosine receptors are divided into two main subtypes (Stiles, 1986). The A1 subtype (A1AR) is inhibitory to adenylate cyclase and exhibits an agonist potency order where R-PIA > NECA > S-PIA. The rapid accumulation of information concerning the structure, function and regulation of the A1AR can be directly attributed to the development of a large number of selective, high affinity radioligands, photoaffinity and affinity probes for this receptor subtype. The A2 adenosine receptor (A2AR), in contrast, is stimulatory to adenylate cyclase and exhibits a distinctly different agonist potency order with NECA > R-PIA > S-PIA. In this case, the dearth of useful A2AR probes has lead to an almost complete lack of information on the structure, function and regulation of this physiologically important receptor subtype.
KeywordsAdenylate Cyclase Adenosine Receptor Binding Subunit Affinity Probe Competitive Binding Experiment
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- Stiles, G.L., 1986, Adenosine receptors: structure, function and regulation in TIPS 7:486–490.Google Scholar