Abstract
Cerebral cannabinoid receptor (CB1) and cannabinoid drugs constitute a vibrant field in modern medicine and pharmacology. However, the physiological and pharmacological roles played by the cannabinoid receptor in the central nervous system are still not fully understood. Positron-emission tomography (PET) is the most advanced technique for non-invasive research of cerebral receptors. Quantitative PET imaging of CB1 in animal and human brains has been limited by drawbacks of the available CB1 radioligands that manifested low specific binding, high non-specific binding and/or low brain uptake. The latest research revealed three CB1 PET radioligands ([ ,C]JHU75528, [ F]MK9470 and [ C]MePPEP) with improved imaging properties. These compounds are now being employed for the quantitative evaluation of CB1 in human subjects with PET. Molecular imaging of the CB1 receptor with these radioligands has now become possible and their application in healthy humans and in patients is underway. Despite the substantial progress in development of CB1 PET radioligands even the latest radioligands manifest certain disadvantages. Current research efforts on the development of CB1 radioligands with higher binding potential, greater brain uptake and more optimal brain kinetics.
Current Pharmaceutical Design
Title: Development of Radioligands for In Vivo Imaging of Type 1 Cannabinoid Receptors (CB1) in Human Brain
Volume: 14 Issue: 31
Author(s): Andrew G. Horti and Koen Van Laere
Affiliation:
Abstract: Cerebral cannabinoid receptor (CB1) and cannabinoid drugs constitute a vibrant field in modern medicine and pharmacology. However, the physiological and pharmacological roles played by the cannabinoid receptor in the central nervous system are still not fully understood. Positron-emission tomography (PET) is the most advanced technique for non-invasive research of cerebral receptors. Quantitative PET imaging of CB1 in animal and human brains has been limited by drawbacks of the available CB1 radioligands that manifested low specific binding, high non-specific binding and/or low brain uptake. The latest research revealed three CB1 PET radioligands ([ ,C]JHU75528, [ F]MK9470 and [ C]MePPEP) with improved imaging properties. These compounds are now being employed for the quantitative evaluation of CB1 in human subjects with PET. Molecular imaging of the CB1 receptor with these radioligands has now become possible and their application in healthy humans and in patients is underway. Despite the substantial progress in development of CB1 PET radioligands even the latest radioligands manifest certain disadvantages. Current research efforts on the development of CB1 radioligands with higher binding potential, greater brain uptake and more optimal brain kinetics.
Export Options
About this article
Cite this article as:
Horti G. Andrew and Laere Van Koen, Development of Radioligands for In Vivo Imaging of Type 1 Cannabinoid Receptors (CB1) in Human Brain, Current Pharmaceutical Design 2008; 14 (31) . https://dx.doi.org/10.2174/138161208786549380
DOI https://dx.doi.org/10.2174/138161208786549380 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
?Revolutionizing Cancer Treatment: Nano-Therapeutics Targeting Tumor Microenvironment?
This thematic issue explores the forefront of cancer treatment, centering on the groundbreaking potential of nano-therapeutics meticulously designed to target the tumor microenvironment. At its core, the issue aims to unravel the latest advancements in nanotechnology, showcasing innovative materials, formulations, and delivery systems that hold promise for redefining cancer therapeutics. ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...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
-
Ionotropic Glutamate Receptor Biology: Effect on Synaptic Connectivity and Function in Neurological Disease
Current Medicinal Chemistry Neuro-Transmitters in the Central Nervous System & their Implication in Learning and Memory Processes
Current Medicinal Chemistry Neuroinflamm-Aging and Neurodegenerative Diseases: An Overview
CNS & Neurological Disorders - Drug Targets Role of Sirtuins and Calorie Restriction in Neuroprotection: Implications in Alzheimers and Parkinsons Diseases
Current Pharmaceutical Design Cancer Nanotechnology: Emerging Role of Gold Nanoconjugates
Anti-Cancer Agents in Medicinal Chemistry Assessing Structure, Function and Druggability of Major Inhibitory Neurotransmitter γ-Aminobutyrate Symporter Subtypes
Current Medicinal Chemistry Investigation and Need of Bioequivalence Study: Methodology and Regulatory Requirement
Applied Clinical Research, Clinical Trials and Regulatory Affairs Astrocytic Target Mechanisms in Epilepsy
Current Medicinal Chemistry Renin-Angiotensin System in Central Nervous System Diseases and its Interaction with COVID-19
Current Medicinal Chemistry Patients Stratification Strategies to Optimize the Effectiveness of Scavenging Biogenic Aldehydes: Towards a Neuroprotective Approach for Parkinson's Disease
Current Neuropharmacology Ubiquitin-Protein Ligases - Novel Therapeutic Targets?
Current Protein & Peptide Science New Hopes in Cancer Battle - A Review of New Molecules and Treatment Strategies
Medicinal Chemistry Potential Mechanisms Involved in the Anticonvulsant Effect of Methanol Extract of <i>Pyrenancantha staudtii</i> in Mice
Central Nervous System Agents in Medicinal Chemistry Adult Hippocampal Neurogenesis as Target for the Treatment of Depression
CNS & Neurological Disorders - Drug Targets Needle in a Haystack: Targeting Specific Glucuronidases Amid the Human Microbiome
Current Enzyme Inhibition The DREAM of Pain Relief
Current Rheumatology Reviews New Therapeutic Strategies in Perinatal Stroke
Current Drug Targets - CNS & Neurological Disorders Advances in Pediatric Epilepsy Surgery
Current Pediatric Reviews Cardioembolic Stroke: Clinical Features, Specific Cardiac Disorders and Prognosis
Current Cardiology Reviews Drug-Resistant Epilepsy and Surgery
Current Neuropharmacology