Abstract
The adenosine A2A receptor (A2AR) is highly concentrated in the striatum, and a therapeutic target for Parkinson’s disorder (PD) and Huntington’s disease. High affinity and selective radiolabeled A2AR antagonists can be important research and diagnostic tools for PD. Positron Emission Tomography (PET) can play an important role by measuring radiolabeled A2A antagonists non-invasively in the brain. However, till date no complete review on A2AR PET ligands is available. The present article has been therefore focused on available PET tracers for A2AR and their detailed biological evaluation in rodents, nonhuman primates and humans. Drug design and development by molecular modeling including new lead structures that are potential candidates for radiolabeling and mapping of cerebral A2ARs is discussed in the present article. A brief overview of functions of adenosine in health and disease, including the relevance of A2AR for PD has also been presented.
Keywords: Adenosine A2A receptor, Parkinson’s disorder, positron emission tomography (PET), xanthine ligands, nonxanthine ligands, SCH442416, TMSX, 6-OHDA PD model.
Current Medicinal Chemistry
Title:Adenosine A2A Receptor Antagonists as Positron Emission Tomography (PET) Tracers
Volume: 21 Issue: 3
Author(s): S. Khanapur, A. van Waarde, K. Ishiwata, K. L. Leenders, R. A.J.O. Dierckx and P. H. Elsinga
Affiliation:
Keywords: Adenosine A2A receptor, Parkinson’s disorder, positron emission tomography (PET), xanthine ligands, nonxanthine ligands, SCH442416, TMSX, 6-OHDA PD model.
Abstract: The adenosine A2A receptor (A2AR) is highly concentrated in the striatum, and a therapeutic target for Parkinson’s disorder (PD) and Huntington’s disease. High affinity and selective radiolabeled A2AR antagonists can be important research and diagnostic tools for PD. Positron Emission Tomography (PET) can play an important role by measuring radiolabeled A2A antagonists non-invasively in the brain. However, till date no complete review on A2AR PET ligands is available. The present article has been therefore focused on available PET tracers for A2AR and their detailed biological evaluation in rodents, nonhuman primates and humans. Drug design and development by molecular modeling including new lead structures that are potential candidates for radiolabeling and mapping of cerebral A2ARs is discussed in the present article. A brief overview of functions of adenosine in health and disease, including the relevance of A2AR for PD has also been presented.
Export Options
About this article
Cite this article as:
Khanapur S., Waarde van A., Ishiwata K., Leenders L. K., Dierckx A.J.O. R. and Elsinga H. P., Adenosine A2A Receptor Antagonists as Positron Emission Tomography (PET) Tracers, Current Medicinal Chemistry 2014; 21 (3) . https://dx.doi.org/10.2174/09298673113206660265
DOI https://dx.doi.org/10.2174/09298673113206660265 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
-
Therapeutic Strategies Targeting Endothelial Function in Humans:Clinical Implications
Current Vascular Pharmacology Air Pollution Exposure and Blood Pressure: An Updated Review of the Literature
Current Pharmaceutical Design Surgical Treatment of Neonatal Mastitis by Periareolar Drainage
Current Pediatric Reviews Microcirculation of the Diabetic Foot
Current Pharmaceutical Design Role of Diagnostic Ultrasound in Patient Selection for Stroke Intervention
Recent Patents on CNS Drug Discovery (Discontinued) Mitochondria-Targeted Drugs
Current Molecular Pharmacology Endothelial (Dys)Function in Lone Atrial Fibrillation
Current Pharmaceutical Design Synthesis and Biological Evaluation of Novel Pyrazole Derivatives as Anti-Inflammatory Antimicrobial Agents
Medicinal Chemistry Pregnancy and Sleep Apnea
Current Respiratory Medicine Reviews Recent Patents and Emerging Therapeutics in the Treatment of Allergic Conjunctivitis
Recent Patents on Inflammation & Allergy Drug Discovery Oxidative Stress Induced Mitochondrial DNA Deletion as a Hallmark forthe Drug Development in the Context of the Cerebrovascular Diseases
Recent Patents on Cardiovascular Drug Discovery Ezetimibe and Reactive Oxygen Species
Current Vascular Pharmacology Imaging Patterns of Cardiovascular Involvement in Mixed Connective Tissue Disease Evaluated by Cardiovascular Magnetic Resonance
Inflammation & Allergy - Drug Targets (Discontinued) Neurovascular Changes in Acute, sub-Acute and Chronic Mouse Models of Parkinson’s Disease
Current Neurovascular Research Role of Sensory Neurons in Restitution and Healing of Gastric Ulcers
Current Pharmaceutical Design Mediterranean Diet Rich in Olive Oil and Obesity, Metabolic Syndrome and Diabetes Mellitus
Current Pharmaceutical Design Pathogenesis of Acute Kidney Injury During Sepsis
Current Drug Targets Computed Tomography Imaging of the Coronary Arteries: State of the Art Applications and Recent Patents
Recent Patents on Medical Imaging Transcranial Doppler Ultrasonography: Current Status
Current Medical Imaging Recent Advances in the Treatment of Neurogenic Erectile Dysfunction
Recent Patents on CNS Drug Discovery (Discontinued)