Abstract
Serotonin and its various receptors are involved in numerous brain functions and neuropsychiatric disorders. The 5-HT1A family is the best characterized subtype of the fourteen currently known 5-HT receptors. The 5-HT1A receptor is closely involved in the pathogenesis of anxiety, depression, epilepsy and eating disorders and therefore is an important target for drug therapy. The development in the 1980s of molecules specifically targeting this receptor was followed by the rapid development of corresponding PET neuroimaging. Because this receptor represents a crucial target in neuroscience, a large number of radioligands have been developed by academic and industry centers for visualization and quantification, first in living animals and ultimately in humans. After a brief account of some of the structural and functional characteristics of brain 5-HT1A receptors, this review focuses on the main lines of evolutionopened up by preclinical and clinical 5-HT1A PET radiopharmaceuticals, illustrating the potential value of PET for clinical research and drug development.
Keywords: Agonist, antagonist, neurotransmission, positron emission tomography, radiopharmaceutical, 5-HT1A receptor.
Current Medicinal Chemistry
Title:PET Radiotracers for Molecular Imaging of Serotonin 5-HT1A Receptors
Volume: 21 Issue: 1
Author(s): T. Billard, D. Le Bars and L. Zimmer
Affiliation:
Keywords: Agonist, antagonist, neurotransmission, positron emission tomography, radiopharmaceutical, 5-HT1A receptor.
Abstract: Serotonin and its various receptors are involved in numerous brain functions and neuropsychiatric disorders. The 5-HT1A family is the best characterized subtype of the fourteen currently known 5-HT receptors. The 5-HT1A receptor is closely involved in the pathogenesis of anxiety, depression, epilepsy and eating disorders and therefore is an important target for drug therapy. The development in the 1980s of molecules specifically targeting this receptor was followed by the rapid development of corresponding PET neuroimaging. Because this receptor represents a crucial target in neuroscience, a large number of radioligands have been developed by academic and industry centers for visualization and quantification, first in living animals and ultimately in humans. After a brief account of some of the structural and functional characteristics of brain 5-HT1A receptors, this review focuses on the main lines of evolutionopened up by preclinical and clinical 5-HT1A PET radiopharmaceuticals, illustrating the potential value of PET for clinical research and drug development.
Export Options
About this article
Cite this article as:
Billard T., Bars Le D. and Zimmer L., PET Radiotracers for Molecular Imaging of Serotonin 5-HT1A Receptors, Current Medicinal Chemistry 2014; 21 (1) . https://dx.doi.org/10.2174/09298673113209990215
DOI https://dx.doi.org/10.2174/09298673113209990215 |
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
-
Effect of Levetiracetam on Cognitive Function and Clonic Seizure Frequency in Children with Epilepsy
Current Molecular Medicine Histamine H3 Receptor Function and Ligands: Recent Developments
Mini-Reviews in Medicinal Chemistry Iptakalim Hydrochloride and Neuronal Protection
Current Neuropharmacology Preface
Current Drug Targets - CNS & Neurological Disorders Autoimmune Diabetes Mellitus: The Importance of Autoantibodies for Disease Prediction and Diagnostic Support
Current Immunology Reviews (Discontinued) Preface
Current Drug Targets - CNS & Neurological Disorders Recent Progress in Research on Ribosome Inactivating Proteins
Current Protein & Peptide Science Current Options in the Treatment of Mitochondrial Diseases
Recent Patents on CNS Drug Discovery (Discontinued) Delirium Secondary to Lamotrigine Toxicity
Current Drug Safety Drug Delivery to CNS: Challenges and Opportunities with Emphasis on Biomaterials Based Drug Delivery Strategies
Current Pharmaceutical Design Targeting of Peripherally Expressed Pain-Related Molecules in Injury- Induced Chronic Neuropathic Pain
CNS & Neurological Disorders - Drug Targets Are Carbonic Anhydrase Inhibitors Suitable for Obtaining Antiobesity Drugs ?
Current Pharmaceutical Design Diacylglycerol Kinases as Emerging Potential Drug Targets for a Variety of Diseases
Current Drug Targets 2,3-Disubtituted Thiazolidin-4-ones: Novel Class of Anticonvulsant Agents
Letters in Drug Design & Discovery Understanding Membrane Protein Drug Targets in Computational Perspective
Current Drug Targets Therapeutic Options in Prevention and Treatment of Aspartoacylase Gene Mutation Resulting Abnormalities in Canavan Disease
Current Pharmacogenomics Targeting BLyS in Systemic Lupus Erythematosus
Recent Patents on Inflammation & Allergy Drug Discovery Acid-Sensing Ion Channels Structural Aspects, Pathophysiological Importance and Experimental Mutational Data Available Across Various Species to Target Human ASIC1
Current Drug Targets Standardization Using Analytical Techniques (UV, NMR, FTIR, HPLC, Mass) and Pharmacognostic Evaluation of the Roots of <i>Selinum vaginatum</i>: A Rare Himalayan Plant of the Rohtang Region
Current Biotechnology Computational Drug Repositioning: A Lateral Approach to Traditional Drug Discovery?
Current Topics in Medicinal Chemistry