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Identification of the A2 Adenosine Receptor Binding Subunit by Photoaffinity Crosslinking

  • W. W. Barrington
  • K. A. Jacobson
  • A. J. Hutchison
  • M. Williams
  • G. L. Stiles
Conference paper

Abstract

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.

Keywords

Adenylate Cyclase Adenosine Receptor Binding Subunit Affinity Probe Competitive Binding Experiment 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

  1. Barrington, W.W., Jacobson, K.A., Hutchison, A.J., Williams, M., and Stiles, G.L., 1989, Identification of the A2 adenosine receptor binding subunit by photoaffinity crosslinking, in Proc. Natl. Acad. Sci. USA 86:6572–6576.PubMedCrossRefGoogle Scholar
  2. Bruns, R.F., Lu, G.H., and Pugsley, T.A., 1986, Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes, in Mol. Pharmacol. 29:331–346.PubMedGoogle Scholar
  3. Stiles, G.L., 1986, Adenosine receptors: structure, function and regulation in TIPS 7:486–490.Google Scholar
  4. Stiles, G.L., and Jacobson, K.A., 1987, A new high affinity, iodinated adenosine receptor antagonist as a radioligand/photoaffinity crosslinking probe, in Mol. Pharmacol. 32:184–188.PubMedGoogle Scholar

Copyright information

© Springer-Verlag New York Inc. 1990

Authors and Affiliations

  • W. W. Barrington
  • K. A. Jacobson
  • A. J. Hutchison
  • M. Williams
  • G. L. Stiles

There are no affiliations available

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