Abstract
Adenosine A2A receptors are members of the G protein-coupled receptor family and mediate multiple physiological effects of adenosine, both at the central nervous system (CNS) and at peripheral tissues, by activating several pathways or interacting with other receptors or proteins. Increasing evidence relate A2A receptors with pharmacological stress testing, neurodegenerative disorders (such as Parkinsons disease) and inflammation, renewing the interest in these receptors, increasingly viewed as promising therapeutic targets. Series of agonists and antagonists have been developed by medicinal chemistry artwork either by structure activity relationship (SAR) or quantitative structure activity relationship (QSAR) studies. These studies have allowed identification of the structural and electrostatic requirements for high affinity A2A receptor binding and, therefore, contributing to the rational design of A2A receptor ligands. Additional rational chemical modifications of the existing A2A receptor ligands may further improve their affinity/selectivity. The purpose of this review is to analize and summarize aspects related to the medicinal chemistry of A2A receptor ligands, their present and potencial therapeutic applications by exploring the molecular structure and physiological and pathophysiological roles of A2A receptors.
Keywords: A2A receptor ligands, modified nucleosides, modified purines, other heterocycles, synthetic strategies, A2A receptor antagonists, A2A receptor agonists
Current Pharmaceutical Design
Title: Ligands and Therapeutic Perspectives of Adenosine A2A Receptors
Volume: 14 Issue: 17
Author(s): C. Diniz, F. Borges, L. Santana, E. Uriarte, J. M.A. Oliveira, J. Goncalves and P. Fresco
Affiliation:
Keywords: A2A receptor ligands, modified nucleosides, modified purines, other heterocycles, synthetic strategies, A2A receptor antagonists, A2A receptor agonists
Abstract: Adenosine A2A receptors are members of the G protein-coupled receptor family and mediate multiple physiological effects of adenosine, both at the central nervous system (CNS) and at peripheral tissues, by activating several pathways or interacting with other receptors or proteins. Increasing evidence relate A2A receptors with pharmacological stress testing, neurodegenerative disorders (such as Parkinsons disease) and inflammation, renewing the interest in these receptors, increasingly viewed as promising therapeutic targets. Series of agonists and antagonists have been developed by medicinal chemistry artwork either by structure activity relationship (SAR) or quantitative structure activity relationship (QSAR) studies. These studies have allowed identification of the structural and electrostatic requirements for high affinity A2A receptor binding and, therefore, contributing to the rational design of A2A receptor ligands. Additional rational chemical modifications of the existing A2A receptor ligands may further improve their affinity/selectivity. The purpose of this review is to analize and summarize aspects related to the medicinal chemistry of A2A receptor ligands, their present and potencial therapeutic applications by exploring the molecular structure and physiological and pathophysiological roles of A2A receptors.
Export Options
About this article
Cite this article as:
Diniz C., Borges F., Santana L., Uriarte E., Oliveira M.A. J., Goncalves J. and Fresco P., Ligands and Therapeutic Perspectives of Adenosine A2A Receptors, Current Pharmaceutical Design 2008; 14 (17) . https://dx.doi.org/10.2174/138161208784746842
DOI https://dx.doi.org/10.2174/138161208784746842 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- 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
-
Apoptosis-Inducing Effects of Amaryllidaceae Alkaloids
Current Medicinal Chemistry SUMOylation in Neurological Diseases
Current Molecular Medicine Novel Anti-Inflammatory and Neuroprotective Agents for Parkinsons Disease
CNS & Neurological Disorders - Drug Targets A Novel Approach for Substitution of Sulfonate Group by (1H)-imidazole moiety: An Application for Synthesis of Novel Benzyl Imidazolyl carbamates
Letters in Organic Chemistry Doppler Haemodynamics of Cerebral Venous Return
Current Neurovascular Research Therapeutic Strategies Targeting Amyloid-β in Alzheimer’s Disease
Current Alzheimer Research Amyloid β Oligomers Decrease Hippocampal Spontaneous Network Activity in an Age-Dependent Manner
Current Alzheimer Research Stem Cells as a Potential Therapeutic Option for Treating Neurodegenerative Diseases
Current Stem Cell Research & Therapy Drugs Polypharmacology by In Silico Methods: New Opportunities in Drug Discovery
Current Pharmaceutical Design Targeting Histone Deacetylases for the Treatment of Immune, Endocrine & Metabolic Disorders
Endocrine, Metabolic & Immune Disorders - Drug Targets Therapeutic Perspectives of Drugs Targeting Toll-Like Receptors Based on Immune Physiopathology Theory of Alzheimers Disease
CNS & Neurological Disorders - Drug Targets Microglia and Astrocytes in Alzheimer's Disease: Implications for Therapy
Current Neuropharmacology Cultured Adult Animal Neurons and Schwann Cells Give Us New Insights into Diabetic Neuropathy
Current Diabetes Reviews Oxidative Stress and NAD+ in Ischemic Brain Injury: Current Advances and Future Perspectives
Current Medicinal Chemistry Targeted Drug Delivery in Brain Tumors-nanochemistry Applications and Advances
Current Topics in Medicinal Chemistry Innovative Therapeutic Potential of Cannabinoid Receptors as Targets in Alzheimer’s Disease and Less Well-Known Diseases
Current Medicinal Chemistry Current Antioxidant Molecular Therapies for Oxidative Stress-Related Ailments
Current Gene Therapy Protective Effects of Caffeic Acid and the Alzheimer's Brain: An Update
Mini-Reviews in Medicinal Chemistry Nanoparticles: A Neurotoxicological Perspective
CNS & Neurological Disorders - Drug Targets CRISPR-Cas Technology: A Role in Transcriptional Recording and Chromatin Remodeling Events
Current Chemical Biology