Naunyn-Schmiedeberg's Archives of Pharmacology

, Volume 362, Issue 4, pp 382–391

Adenosine receptors and their ligands

  • Karl-Norbert Klotz
Review Article

DOI: 10.1007/s002100000315

Cite this article as:
Klotz, KN. Naunyn-Schmied Arch Pharmacol (2000) 362: 382. doi:10.1007/s002100000315


The regulatory actions of adenosine are mediated via four subtypes of G protein-coupled receptors distinguished as A1, A2A, A2B and A3 receptors. Their presence on basically every cell makes them an interesting target for the pharmacological intervention in many pathophysiological situations. A large number of ligands have been synthesized over the last two decades and provide agonists and antagonists that are more or less selective for the known receptor subtypes. In addition, many radioligands are available in tritiated or radioiodinated form. The comparative pharmacological characterization of all four human adenosine receptor subtypes revealed that some of the compounds thought to be selective from data in other species have unexpected potencies at human receptors. As a result, compounds that exhibit high affinity to only one subtype are an exception. Although the selection of ligands is immense, it is less than satisfying for most subtypes of adenosine receptors.

Adenosine Adenosine receptors Agonist Antagonist Selectivity High affinity A1 A2A A2B A3 Ligand Radioligand Human 

Copyright information

© Springer-Verlag 2000

Authors and Affiliations

  • Karl-Norbert Klotz
    • 1
  1. 1.Institut für Pharmakologie und Toxikologie, Universität Würzburg, Versbacher Strasse 9, D-97078 WürzburgGermany

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