Recent developments in adenosine receptor ligands and their potential as novel drugs.

Abstract

Medicinal chemical approaches have been applied to all four of the adenosine receptor (AR) subtypes (A(1), A(2A), A(2B), and A(3)) to create selective agonists and antagonists for each. The most recent class of selective AR ligands to be reported is the class of A(2B)AR agonists. The availability of these selective ligands has facilitated research on therapeutic applications of modulating the ARs and in some cases has provided clinical candidates. Prodrug approaches have been developed which improve the bioavailability of the drugs, reduce side-effects, and/or may lead to site-selective effects. The A(2A) agonist regadenoson (Lexiscan®), a diagnostic drug for myocardial perfusion imaging, is the first selective AR agonist to be approved. Other selective agonists and antagonists are or were undergoing clinical trials for a broad range of indications, including capadenoson and tecadenoson (A(1) agonists) for atrial fibrillation, or paroxysmal supraventricular tachycardia, respectively, apadenoson and binodenoson (A(2A) agonists) for myocardial perfusion imaging, preladenant (A(2A) antagonist) for the treatment of Parkinson's disease, and CF101 and CF102 (A(3) agonists) for inflammatory diseases and cancer, respectively.

• Authors: Christa E Müller, Kenneth A Jacobson
• Journal: Biochimica et biophysica acta (Biochim Biophys Acta) Vol. 1808 Issue 5 Pg. 1290-308 (May 2011) ISSN: 0006-3002 [Print] Netherlands
• PMID: 21185259 (Publication Type: Journal Article, Research Support, N.I.H., Intramural, Review)
• Copyright: Copyright © 2010 Elsevier B.V. All rights reserved.

Chemical References

• Ligands
• Purinergic P1 Receptor Agonists
• Purinergic P1 Receptor Antagonists
• Receptors, Purinergic P1

Topics

• Animals
• Drug Design
• Humans
• Ligands
• Protein Binding
• Purinergic P1 Receptor Agonists (metabolism)
• Purinergic P1 Receptor Antagonists (metabolism)
• Receptors, Purinergic P1 (chemistry, metabolism)