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
Export Options
About this article
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
C. elegans as a Genetic Model System to Identify Parkinson's Disease- Associated Therapeutic Targets
CNS & Neurological Disorders - Drug Targets Effect of Trichostatin A on Gelsolin Levels, Proteolysis of Amyloid Precursor Protein, and Amyloid Beta-Protein Load in the Brain of Transgenic Mouse Model of Alzheimer's Disease
Current Alzheimer Research Preclinical Safety and Pharmacokinetic Profile of 3K3A-APC, a Novel, Modified Activated Protein C for Ischemic Stroke
Current Pharmaceutical Design Neurotrophic Factors as a Protective Strategy in Parkinsons Disease
CNS & Neurological Disorders - Drug Targets Synthesis, Biological Activity of Thiazolidinones Bearing Indoline Moiety and Isatin Based Hybrids
Mini-Reviews in Organic Chemistry Impaired Insulin Sensitivity and Secretion in Patients with Alzheimer’s Disease: The Relationship with Other Atherosclerosis Risk Factors
Current Vascular Pharmacology Regulation and Quantification of Cellular Mitochondrial Morphology and Content
Current Pharmaceutical Design Neuroprotective Role of Natural Polyphenols
Current Topics in Medicinal Chemistry Targeting SUMOylation Cascade for Diabetes Management
Current Drug Targets G-Lymphatic, Vascular and Immune Pathways for Aβ Clearance Cascade and Therapeutic Targets For Alzheimer’s Disease
Combinatorial Chemistry & High Throughput Screening Looking Towards New Pathogenetic Mechanisms in Parkinson’s Disease: is ANT1 the Potential Candidate?
Current Aging Science Oral Health in Alzheimers Disease: A Review
Current Alzheimer Research Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging
Current Medicinal Chemistry Advancing Drug Therapy for Brain Tumours: A Current Review of the Pro-inflammatory Peptide Substance P and its Antagonists as Anti-cancer Agents
Recent Patents on CNS Drug Discovery (Discontinued) Plant Secondary Metabolites- Potent Inhibitors of Monoamine Oxidase Isoforms
Central Nervous System Agents in Medicinal Chemistry Nucleic Acid Therapeutics in Huntington’s Disease
Recent Patents on Biotechnology Parkinson’s Disease: Alpha Synuclein, Heme Oxygenase and Biotherapeutic Countermeasures
Current Pharmaceutical Design The Emory Chemical Biology Discovery Center: Leveraging Academic Innovation to Advance Novel Targets through HTS and Beyond
Combinatorial Chemistry & High Throughput Screening Peripheral Mononuclear Cell Rejuvenation for Senescence Surveillance in Alzheimer Disease
Current Pharmaceutical Design AAVs Anatomy: Roadmap for Optimizing Vectors for Translational Success
Current Gene Therapy