Adenosine receptors in GtoPdb v.2021.2

  • Bertil B. Fredholm Karolinska Institutet
  • Bruno G. Frenguelli University of Warwick
  • Rebecca Hills University of Edinburgh
  • Adriaan P. IJzerman Leiden University https://orcid.org/0000-0002-1182-2259
  • Kenneth A. Jacobson National Institutes of Health https://orcid.org/0000-0001-8104-1493
  • Karl-Norbert Klotz Universität Würzburg
  • Joel Linden La Jolla Institute for Allergy and Immunology
  • Christa E. Müller Universität Bonn
  • Ulrich Schwabe Pharmakologisches Institut der Universität Heidelberg
  • Gary L. Stiles Duke University

Abstract


Adenosine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Adenosine Receptors [110]) are activated by the endogenous ligand adenosine (potentially inosine also at A3 receptors). Crystal structures for the antagonist-bound [153, 313, 221, 61], agonist-bound [375, 203, 204] and G protein-bound A2A adenosine receptors [49] have been described. The structures of an antagonist-bound A1 receptor [128] and an adenosine-bound A1 receptor-Gi complex [86] have been resolved by cryo-electronmicroscopy. Another structure of an antagonist-bound A1 receptor obtained with X-ray crystallography has also been reported [57]. caffeine is a nonselective antagonist for adenosine receptors, while istradefylline, a selective A2A receptor antagonist, is on the market for the treatment of Parkinson's disease.

Published
25-Jun-2021
How to Cite
Fredholm, B. B., Frenguelli, B. G., Hills, R., IJzerman, A. P., Jacobson, K. A., Klotz, K.-N., Linden, J., Müller, C. E., Schwabe, U. and Stiles, G. L. (2021) “Adenosine receptors in GtoPdb v.2021.2”, IUPHAR/BPS Guide to Pharmacology CITE, 2021(2). doi: 10.2218/gtopdb/F3/2021.2.
Section
Summaries