Abstract
The dopaminergic system plays a major role in neurological and psychiatric disorders such as Parkinsons disease, Huntingtons disease, tardive dyskinea and schizophrenia. Knowledge on altered dopamine synthesis, receptor densities and status are important for understanding the mechanisms underlying the pathogenesis and therapy of diseases. PET provides a non-invasive tool to investigate these features in vivo, provided the availability of suitable radiopharmaceuticals. To investigate presynaptic function, PET-tracers have been developed to measure dopamine synthesis and transport. For the former the most commonly used tracers are 6-[18F]FDOPA and 6-[18F]FMT, whereas for the latter several 11C/18F-labeled tropane analogues are being clinically used. Postsynaptically, dopamine exerts actions through several subtypes of the dopamine receptor. The dopamine receptor family consists of 5 subtypes D1-D5. In order to investigate the role of each receptor subtype, selective and high-affinity PETradioligands are required. For the dopamine D1-subtype the most commonly used ligand is [11C]SCH 23390 or [11C]NNC 112, whereas for the D2/D3-subtype [11C]raclopride is a common tracer. [18 F]Fallypride is a suitable PET-tracer for the investigation of extrapyramidal D2-receptors. For the other subtypes no suitable radioligands have been developed yet. This paper gives an overview of the current status on dopamine PET-tracers and the development of new lead compounds as potential PET-tracers by medicinal chemistry.
Keywords: positron emission tomography, dopamine receptor, dopamine transporter, Dopamine synthesis
Current Medicinal Chemistry
Title: PET Tracers for Imaging of the Dopaminergic System
Volume: 13 Issue: 18
Author(s): Kentaro Hatano, Kiichi Ishiwata and Philip H. Elsinga
Affiliation:
Keywords: positron emission tomography, dopamine receptor, dopamine transporter, Dopamine synthesis
Abstract: The dopaminergic system plays a major role in neurological and psychiatric disorders such as Parkinsons disease, Huntingtons disease, tardive dyskinea and schizophrenia. Knowledge on altered dopamine synthesis, receptor densities and status are important for understanding the mechanisms underlying the pathogenesis and therapy of diseases. PET provides a non-invasive tool to investigate these features in vivo, provided the availability of suitable radiopharmaceuticals. To investigate presynaptic function, PET-tracers have been developed to measure dopamine synthesis and transport. For the former the most commonly used tracers are 6-[18F]FDOPA and 6-[18F]FMT, whereas for the latter several 11C/18F-labeled tropane analogues are being clinically used. Postsynaptically, dopamine exerts actions through several subtypes of the dopamine receptor. The dopamine receptor family consists of 5 subtypes D1-D5. In order to investigate the role of each receptor subtype, selective and high-affinity PETradioligands are required. For the dopamine D1-subtype the most commonly used ligand is [11C]SCH 23390 or [11C]NNC 112, whereas for the D2/D3-subtype [11C]raclopride is a common tracer. [18 F]Fallypride is a suitable PET-tracer for the investigation of extrapyramidal D2-receptors. For the other subtypes no suitable radioligands have been developed yet. This paper gives an overview of the current status on dopamine PET-tracers and the development of new lead compounds as potential PET-tracers by medicinal chemistry.
Export Options
About this article
Cite this article as:
Hatano Kentaro, Ishiwata Kiichi and Elsinga H. Philip, PET Tracers for Imaging of the Dopaminergic System, Current Medicinal Chemistry 2006; 13 (18) . https://dx.doi.org/10.2174/092986706777935258
DOI https://dx.doi.org/10.2174/092986706777935258 |
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
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
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
Alzheimer’s Disease and Retinal Degeneration: A Glimpse at Essential Trace Metals in Ocular Fluids and Tissues
Current Alzheimer Research Melatonin Treatment Enhances Aβ Lymphatic Clearance in a Transgenic Mouse Model of Amyloidosis
Current Alzheimer Research Involvement of Mast Cells in Angiogenesis and Chronic Inflammation
Current Drug Targets - Inflammation & Allergy ACKNOWLEDGEMENTS TO REVIEWERS
Current Neuropharmacology Editorial: Upwards and Downwards: Advancing Knowledge in Adolescent Psychiatry
Adolescent Psychiatry Melatonin Causes Gene Expression in Aged Animals to Respond to Inflammatory Stimuli in a Manner Differing from that of Young Animals
Current Aging Science Deciphering the Physiology Underlying the Rapid Clinical Effects of Perispinal Etanercept in Alzheimers Disease
Current Alzheimer Research Development of MLR and SVM Aided QSAR Models to Identify Common SAR of GABA Uptake Herbal Inhibitors used in the Treatment of Schizophrenia
Current Neuropharmacology Concurrent Estimation of Gabapentin and Nortriptyline Hydrochloride in their Combined Dosage Form Using OPA-β-Mercaptoethanol Derivatization by Spectrophotometric and Spectrofluorimetric Methods
Current Pharmaceutical Analysis The Protective Effects of Jatrorrhizine on β-Amyloid (25-35)-Induced Neurotoxicity in Rat Cortical Neurons
CNS & Neurological Disorders - Drug Targets The Neural Basis of Three Elements in Language Processing: A Review of Neuroimaging Studies
Neuroscience and Biomedical Engineering (Discontinued) Recent Applications of Microwaves in Synthesis of Bioactive Heterocyclic Compounds
Current Organic Chemistry Chemical Composition, Antioxidant, Alpha-glucosidase Inhibitory, Anticholinesterase and Photoprotective Activities of the Aerial Parts of <i>Schinus molle</i> L.
Current Bioactive Compounds The Interaction of Zinc Oxide/Green Tea Extract Complex Nanoparticles and its Effect on Monosodium Glutamate Toxicity in Liver of Rats
Current Pharmaceutical Biotechnology Concept of Comprehensive Treatment for Osteoarthritis (OA)
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents DNA Methylation Markers in Lung Cancer
Current Genomics Predicting Dopamine Receptors Binding Affinity of N-[4-(4-Arylpiperazin- 1-yl) butyl]Aryl Carboxamides: Computational Approach Using Topological Descriptors
Current Drug Discovery Technologies Beyond Rodent Models of Pain: Non-Human Primate Models for Evaluating Novel Analgesic Therapeutics and Elaborating Pain Mechanisms
CNS & Neurological Disorders - Drug Targets Biomarker-Guided Strategy for Treatment of Autism Spectrum Disorder (ASD)
CNS & Neurological Disorders - Drug Targets Future Targets in Endometriosis Treatment: Targeting the Endometriotic Implant
Mini-Reviews in Medicinal Chemistry