Abstract
Serotonin receptors (5-HTRs) are implicated in the pathophysiology of a variety of neuropsychiatric and neurodegenerative disorders and are also targets for drug therapy. In the CNS, most of these receptors are expressed in high abundance in specific brain regions reflecting their role in brain functions. Quantifying binding to 5-HTRs in vivo may permit assessment of physiologic and pathologic conditions, and monitoring disease progression, evaluating treatment response, and for investigating new treatment modalities. Positron emission tomography (PET) molecular imaging has the sensitivity to quantify binding of 5-HTRs in CNS disorders and to measure drug occupancy as part of a process of new drug development. Although research on PET imaging of 5-HTRs have been performed more than two decades, the successful radiotracers so far developed for human studies are limited to 5-HT1AR, 5-HT1BR, 5-HT2AR, 5-HT4R and 5-HT6R. Herein we review the development and application of radioligands for PET imaging of 5-HTRs in living brain.
Keywords: Molecular imaging, PET, 5-HTR, radioligands, serotonin receptors.
Central Nervous System Agents in Medicinal Chemistry
Title:PET Tracers for Serotonin Receptors and Their Applications
Volume: 14 Issue: 2
Author(s): J.S. Dileep Kumar and J. John Mann
Affiliation:
Keywords: Molecular imaging, PET, 5-HTR, radioligands, serotonin receptors.
Abstract: Serotonin receptors (5-HTRs) are implicated in the pathophysiology of a variety of neuropsychiatric and neurodegenerative disorders and are also targets for drug therapy. In the CNS, most of these receptors are expressed in high abundance in specific brain regions reflecting their role in brain functions. Quantifying binding to 5-HTRs in vivo may permit assessment of physiologic and pathologic conditions, and monitoring disease progression, evaluating treatment response, and for investigating new treatment modalities. Positron emission tomography (PET) molecular imaging has the sensitivity to quantify binding of 5-HTRs in CNS disorders and to measure drug occupancy as part of a process of new drug development. Although research on PET imaging of 5-HTRs have been performed more than two decades, the successful radiotracers so far developed for human studies are limited to 5-HT1AR, 5-HT1BR, 5-HT2AR, 5-HT4R and 5-HT6R. Herein we review the development and application of radioligands for PET imaging of 5-HTRs in living brain.
Export Options
About this article
Cite this article as:
Kumar Dileep J.S. and Mann John J., PET Tracers for Serotonin Receptors and Their Applications, Central Nervous System Agents in Medicinal Chemistry 2014; 14 (2) . https://dx.doi.org/10.2174/1871524914666141030124316
DOI https://dx.doi.org/10.2174/1871524914666141030124316 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
- 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
-
Brain Drug Delivery Systems for Neurodegenerative Disorders
Current Pharmaceutical Biotechnology Defective HIF Signaling Pathway and Brain Response to Hypoxia in Neurodegenerative Diseases: Not an “Iffy” Question!
Current Pharmaceutical Design Lipid Alterations in the Earliest Clinically Recognizable Stage of Alzheimers Disease: Implication of the Role of Lipids in the Pathogenesis of Alzheimers Disease
Current Alzheimer Research Histone Deacetylation and Motor Neuron Degeneration
CNS & Neurological Disorders - Drug Targets Nanotechnology and Antioxidant Therapy: An Emerging Approach for Neurodegenerative Diseases
Current Medicinal Chemistry Drug Delivery to CNS: Challenges and Opportunities with Emphasis on Biomaterials Based Drug Delivery Strategies
Current Pharmaceutical Design Targeting the Secretory Pathway for Anti-Inflammatory Drug Development
Current Topics in Medicinal Chemistry Mesenchymal Stromal Cells from Umbilical Cord Blood
Current Stem Cell Research & Therapy Insulin Resistance and Alzheimers Disease: Molecular Links & Clinical Implications
Current Alzheimer Research An Insight into Molecular Mechanisms and Novel Therapeutic Approaches in Epileptogenesis
CNS & Neurological Disorders - Drug Targets Monoamine Oxidase Inhibition and Molecular Modeling Studies of Piperidyl-thienyl and 2-Pyrazoline Derivatives of Chalcones
Medicinal Chemistry Polyisoprenylation Potentiates the Inhibition of Polyisoprenylated Methylated Protein Methyl Esterase and the Cell Degenerative Effects of Sulfonyl Fluorides
Current Cancer Drug Targets Cannabinoids and Neuroprotection in Motor-Related Disorders
CNS & Neurological Disorders - Drug Targets Nanocapsulated Ascorbic Acid in Combating Cerebral Ischemia Reperfusion- Induced Oxidative Injury in Rat Brain
Current Alzheimer Research Neuroprotective Effects of Quercetin: From Chemistry to Medicine
CNS & Neurological Disorders - Drug Targets Innovative Anthocyanin/Anthocyanidin Formulation Protects SK-N-SH Cells Against the Amyloid-β Peptide-Induced Toxicity: Relevance to Alzheimer’s Disease
Central Nervous System Agents in Medicinal Chemistry Biological Predictors of Aging and Potential of FTIR to Study Age-related Diseases and Aging Metabolic Fingerprint
Current Metabolomics Hybrid Molecules Synergistically Acting Against Protein Aggregation Diseases
Current Topics in Medicinal Chemistry The Versatile Stress Protein Mortalin as a Chaperone Therapeutic Agent
Protein & Peptide Letters Enriching One’s Environment in the Face of Cognitive and Functional Loss
Current Neurovascular Research