Journal
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
Volume 1808, Issue 5, Pages 1290-1308Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.bbamem.2010.12.017
Keywords
Adenosine receptor; Agonist; Antagonist; Clinical trial; Medicinal chemistry; G protein-coupled receptor
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Funding
- NIH, National Institute of Diabetes & Digestive & Kidney Diseases
- BMBF (BioPharma - Neuroallianz)
- DFG
- DAAD
- European Commission (ERANET Neuron)
- State of North-Rhine Westfalia (NRW International Research Graduate Schools BIOTECH-PHARMA and Chemical Biology)
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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 (R)), 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. This article is part of a Special Issue entitled: Adenosine Receptors. (C) 2010 Elsevier B.V. All rights reserved.
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