Adenosine A2A receptor as a drug discovery target

J Med Chem. 2014 May 8;57(9):3623-50. doi: 10.1021/jm4011669. Epub 2013 Nov 15.


The adenosine A2A receptor is a G-protein-coupled receptor (GPCR) that has been extensively studied during the past few decades because it offers numerous possibilities for therapeutic applications. Herein we describe adenosine A2A receptor distribution, signaling pathways, pharmacology, and molecular structure, followed by a summary and SAR discussion of the most relevant series of adenosine A2A agonists and antagonists. This review also provides an update of the A2A ligands that are undergoing or have undergone clinical studies, including the two currently marketed agonists adenosine and regadenoson.

Publication types

  • Review

MeSH terms

  • Adenosine A2 Receptor Agonists / pharmacology
  • Adenosine A2 Receptor Agonists / therapeutic use
  • Adenosine A2 Receptor Antagonists / pharmacology
  • Adenosine A2 Receptor Antagonists / therapeutic use
  • Crystallography, X-Ray
  • Drug Discovery*
  • Humans
  • Ligands
  • Protein Conformation
  • Receptor, Adenosine A2A / chemistry
  • Receptor, Adenosine A2A / drug effects*
  • Receptor, Adenosine A2A / metabolism
  • Signal Transduction


  • Adenosine A2 Receptor Agonists
  • Adenosine A2 Receptor Antagonists
  • Ligands
  • Receptor, Adenosine A2A