Abstract
In the central nervous system (CNS) and in the periphery, specific proteins (transporters) are responsible for the regulation of the synaptic concentrations of the major monoamine neurotransmitters, noradrenaline (NE), serotonin (5-HT) and dopamine (DA). Several reports have shown that the expression of these transporters within the CNS may be altered in patients with certain neurodegenerative or neuropsychiatric disorders. Therefore, in the CNS the monoamine transporters are major targets for existing and developmental drugs. The best known drugs targeting these transporters are the selective 5-HT reuptake inhibitors (SSRIs) (e.g. citalopram, Celexa®) that are most frequently used in the treatment of clinical depression. Selective NE reuptake inhibitors (NRIs) have also found use for the treatment of depression and other conditions such as attention deficit hyperactivity (ADHD) disorder. Given that the NE transporter (NET) is also a binding site for cocaine and drugs of abuse, there is a great need for a probe to assess the densities of NET in vivo by brain imaging with either positron emission tomography (PET) or single photon emission tomography (SPET). PET in particular has the potential to measure NET densities quantitatively and with high resolution in the human brain in vivo. The quality of a PET image depends crucially on the radioligand used in the emission measurement. Commonly used radionuclides in PET radioligands are carbon-11 (t1/2 = 20.4 min) and fluorine-18 (t1/2 = 109.8 min). This review specifically summarizes the present status of the development of 11C- or 18F-labeled ligands as tools for imaging NET in brain with PET in support of neuropsychiatric clinical research and drug development.
Keywords: NET, radioligand, PET, carbon-11, fluorine-18
Current Topics in Medicinal Chemistry
Title: Development of Radioligands for Imaging of Brain Norepinephrine Transporters In Vivo with Positron Emission Tomography
Volume: 7 Issue: 18
Author(s): Magnus Schou, Victor W. Pike and Christer Halldin
Affiliation:
Keywords: NET, radioligand, PET, carbon-11, fluorine-18
Abstract: In the central nervous system (CNS) and in the periphery, specific proteins (transporters) are responsible for the regulation of the synaptic concentrations of the major monoamine neurotransmitters, noradrenaline (NE), serotonin (5-HT) and dopamine (DA). Several reports have shown that the expression of these transporters within the CNS may be altered in patients with certain neurodegenerative or neuropsychiatric disorders. Therefore, in the CNS the monoamine transporters are major targets for existing and developmental drugs. The best known drugs targeting these transporters are the selective 5-HT reuptake inhibitors (SSRIs) (e.g. citalopram, Celexa®) that are most frequently used in the treatment of clinical depression. Selective NE reuptake inhibitors (NRIs) have also found use for the treatment of depression and other conditions such as attention deficit hyperactivity (ADHD) disorder. Given that the NE transporter (NET) is also a binding site for cocaine and drugs of abuse, there is a great need for a probe to assess the densities of NET in vivo by brain imaging with either positron emission tomography (PET) or single photon emission tomography (SPET). PET in particular has the potential to measure NET densities quantitatively and with high resolution in the human brain in vivo. The quality of a PET image depends crucially on the radioligand used in the emission measurement. Commonly used radionuclides in PET radioligands are carbon-11 (t1/2 = 20.4 min) and fluorine-18 (t1/2 = 109.8 min). This review specifically summarizes the present status of the development of 11C- or 18F-labeled ligands as tools for imaging NET in brain with PET in support of neuropsychiatric clinical research and drug development.
Export Options
About this article
Cite this article as:
Schou Magnus, Pike W. Victor and Halldin Christer, Development of Radioligands for Imaging of Brain Norepinephrine Transporters In Vivo with Positron Emission Tomography, Current Topics in Medicinal Chemistry 2007; 7 (18) . https://dx.doi.org/10.2174/156802607782507411
DOI https://dx.doi.org/10.2174/156802607782507411 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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 Treatment of Alzheimers Disease Using Metal Complexing Agents
Recent Patents on CNS Drug Discovery (Discontinued) Role of Environmental Contaminants in the Etiology of Alzheimer’s Disease: A Review
Current Alzheimer Research YKL-40 as a Potential Biomarker and a Possible Target in Therapeutic Strategies of Alzheimer’s Disease
Current Neuropharmacology Screening and Analysis of Hypolipidemic Components from Shuangdan Capsule Based on Pancreatic Lipase
Current Bioinformatics Formulation and In Vitro Evaluation of Gelatin Nanospheres for the Oral Delivery of Selegiline
Current Nanoscience Editorial [Hot Topic: Therapeutic Potential of Peptide Motifs - Part II (Executive Editor: Jean-Claude Herve)]
Current Pharmaceutical Design Editorial (Thematic Issue: Myokines and Exercise Training: More Shadows than Lights)
Current Pharmaceutical Design Pathogenic Role of Serine Protease HtrA2/Omi in Neurodegenerative Diseases
Current Protein & Peptide Science Hypercortisolemia and Glucocorticoid Receptor-Signaling Insufficiency in Alzheimer’ s Disease Initiation and Development
Current Alzheimer Research Natural Animal Models of Neurodegenerative Protein Misfolding Diseases
Current Pharmaceutical Design Overlapping the Tryptophan Catabolite (TRYCAT) and Melatoninergic Pathways in Alzheimer's Disease
Current Pharmaceutical Design Turning REST/NRSF Dysfunction in Huntingtons Disease into a Pharmaceutical Target
Current Pharmaceutical Design A New Model for Academics Based Drug Discovery
Current Alzheimer Research Patent Selections
Recent Patents on Inflammation & Allergy Drug Discovery DNAJ Proteins and Protein Aggregation Diseases
Current Topics in Medicinal Chemistry cGAS-STING-mediated IFN-I Response in Host Defense and Neuroinflammatory Diseases
Current Neuropharmacology Drug Targets from Genetics: Alpha-Synuclein
CNS & Neurological Disorders - Drug Targets Design and Development of Novel Transdermal Nanoemulgel for Alzheimer’s Disease: Pharmacokinetic, Pharmacodynamic and Biochemical Investigations
Current Drug Delivery Is Amyloid Binding Alcohol Dehydrogenase a Drug Target for Treating Alzheimer’s Disease?
Current Alzheimer Research Antioxidant Effects of Natural Bioactive Compounds
Current Pharmaceutical Design