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
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
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Transient Receptor Potential Channels - Emerging Novel Drug Targets for the Treatment of Pain
Current Medicinal Chemistry Spectral Investigations, Molecular Interactions and Electrochemical Studies of (2R)-(-)2-(2, 6-dimethylphenylaminocarbonyl)-1-methyl Piperidinium Chloride
Current Drug Therapy Valproic Acid and the Liver Injury in Patients with Epilepsy: An Update
Current Pharmaceutical Design Natural Antioxidants: Therapeutic Prospects for Cancer and Neurological Diseases
Mini-Reviews in Medicinal Chemistry Therapeutic Monitoring of Carbamazepine in Epilepsy Patients by Highly Sensitive LC/MS Method and its Clinical Applications
Current Analytical Chemistry Juvenile Neuronal Ceroid-Lipofuscinosis (Batten Disease): A Brief Review and Update
Current Molecular Medicine Involvement of Potassium and Chloride Channels and Other Transporters in Volume Regulation by Spermatozoa
Current Pharmaceutical Design Molecular and Biochemical Features in Alzheimers Disease
Current Pharmaceutical Design PET Radioligands for In Vivo Visualization of Neuroinflammation
Current Pharmaceutical Design A New Class of Anticonvulsants Possessing 6 Hz Psychomotor Seizure Test Activity: 2-(1H-Benzotriazol-1-yl)-N'-[Substituted] Acetohydrazides
Medicinal Chemistry Caffeine as a Lead Compound for the Design of Therapeutic Agents for the Treatment of Parkinson’s Disease
Current Medicinal Chemistry Role of Unani Medicines in Cancer Control and Management
Current Drug Therapy Neuronal Excitability in Epileptogenic Zones Regulated by the Wnt/ Β-Catenin Pathway
CNS & Neurological Disorders - Drug Targets Naturally Occurring and Related Synthetic Cannabinoids and their Potential Therapeutic Applications
Recent Patents on CNS Drug Discovery (Discontinued) Development and Evaluation of an Anti-Epileptic Oral Fast-Dissolving Film with Enhanced Dissolution and In vivo Permeation
Current Drug Delivery Side Effects of Atypical Antipsychotic Drugs
Current Pharmaceutical Design Potential Implications of Angiotensin-converting Enzyme 2 Blockades on Neuroinflammation in SARS-CoV-2 Infection
Current Drug Targets The FDG-PET Revolution of Medical Imaging – Four Decades and Beyond
Current Molecular Imaging (Discontinued) Natural Products Based Ayurvedic Formulations: Chemical Cons tituents and Treatment in Neurodegenerative Disordersǂ
Mini-Reviews in Organic Chemistry Understanding Effects of Psychological Stress on Physiology and Disease Through Human Stressome - An Integral Algorithm
Current Bioinformatics