Abstract
The adenosine A2A receptor is a member of the G protein-coupled receptor family and mediates multiple physiological effects of adenosine, both at the central nervous system and at peripheral tissues. Increasing evidence relates the A2A receptor with several pathological conditions such as neurodegenerative disorders, inflammation, pharmacological stress, and wound healing renewing the interest in A2A receptor agonists and antagonists as promising leads for drugs. However some of them initially tested in clinical trials presented several side effects, short half-life, lower solubility, and in some cases a lack of effects, perhaps attributable to receptor desensitization or to low receptor density in the targeted tissue. For these reasons it is evident that additional rational chemical modifications of the existing A2A receptor ligands to improve their affinity/selectivity and bioavailability as well as further studies to get new template for A2AAR ligands are necessary. The purpose of this review is to analyze and summarize the past and the present aspects related to the medicinal chemistry of A2A receptor ligands. Moreover their current and possible therapeutic applications have been also highlighted
Keywords: Adenosine, A2A receptor, A2AAR agonist, A2AAR antagonist
Current Topics in Medicinal Chemistry
Title: A2A Receptor Ligands: Past, Present and Future Trends
Volume: 10 Issue: 9
Author(s): C. Manera and G. Saccomanni
Affiliation:
Keywords: Adenosine, A2A receptor, A2AAR agonist, A2AAR antagonist
Abstract: The adenosine A2A receptor is a member of the G protein-coupled receptor family and mediates multiple physiological effects of adenosine, both at the central nervous system and at peripheral tissues. Increasing evidence relates the A2A receptor with several pathological conditions such as neurodegenerative disorders, inflammation, pharmacological stress, and wound healing renewing the interest in A2A receptor agonists and antagonists as promising leads for drugs. However some of them initially tested in clinical trials presented several side effects, short half-life, lower solubility, and in some cases a lack of effects, perhaps attributable to receptor desensitization or to low receptor density in the targeted tissue. For these reasons it is evident that additional rational chemical modifications of the existing A2A receptor ligands to improve their affinity/selectivity and bioavailability as well as further studies to get new template for A2AAR ligands are necessary. The purpose of this review is to analyze and summarize the past and the present aspects related to the medicinal chemistry of A2A receptor ligands. Moreover their current and possible therapeutic applications have been also highlighted
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Cite this article as:
Manera C. and Saccomanni G., A2A Receptor Ligands: Past, Present and Future Trends, Current Topics in Medicinal Chemistry 2010; 10 (9) . https://dx.doi.org/10.2174/156802610791268765
DOI https://dx.doi.org/10.2174/156802610791268765 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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