Abstract
It is important to gain more insight into neurodegenerative diseases, because these debilitating diseases can not be cured. A common characteristic of many neurological diseases is neuroinflammation, which is accompanied by the presence of activated microglia cells. In activated microglia cells, an increase in the expression of peripheral benzodiazepine receptors (PBR) can be found. The PBR was suggested as a target for monitoring disease progression and therapy efficacy with positron emission tomograpy (PET). The PET tracer [ C]PK11195 has been widely used for PBR imaging, but the tracer has a high lipophilicity and high non-specific binding which makes it difficult to quantify uptake. Therefore, efforts are being made to develop more sensitive radioligands for the PBR. Animal studies have yielded several promising new tracers for PBR imaging, such as [ C]DAA1106, [ F]FEDAA1106, [ C]PBR28, [11C]DPA713 and [11C]CLINME. However, the potential of these new PBR ligands is still under investigation and as a consequence [ C]PK11195 is used so far to image activated microglia cells in neurological disorders. With [ C]PK11195, distinct neuroinflammation was detected in multiple sclerosis, Parkinson ’ s disease, encephalitis and other neurological diseases. Because neuroinflammation plays a central role in the progression of neurodegenerative diseases, anti-inflammatory drugs have been investigated for therapeutic intervention. Especially minocycline and cyclooxygenase inhibitors have shown in vivo anti-inflammatory, hence neuroprotective properties, that could be detected by PET imaging of the PBR with [ C]PK11195. The imaging studies published so far showed that the PBR can be an important target for monitoring disease progression, therapy response and determining the optimal drug dose.
Current Pharmaceutical Design
Title: PET Imaging of the Peripheral Benzodiazepine Receptor: Monitoring Disease Progression and Therapy Response in Neurodegenerative Disorders
Volume: 14 Issue: 31
Author(s): Janine Doorduin, Erik F.J. de Vries, Rudi A. Dierckx and Hans C. Klein
Affiliation:
Abstract: It is important to gain more insight into neurodegenerative diseases, because these debilitating diseases can not be cured. A common characteristic of many neurological diseases is neuroinflammation, which is accompanied by the presence of activated microglia cells. In activated microglia cells, an increase in the expression of peripheral benzodiazepine receptors (PBR) can be found. The PBR was suggested as a target for monitoring disease progression and therapy efficacy with positron emission tomograpy (PET). The PET tracer [ C]PK11195 has been widely used for PBR imaging, but the tracer has a high lipophilicity and high non-specific binding which makes it difficult to quantify uptake. Therefore, efforts are being made to develop more sensitive radioligands for the PBR. Animal studies have yielded several promising new tracers for PBR imaging, such as [ C]DAA1106, [ F]FEDAA1106, [ C]PBR28, [11C]DPA713 and [11C]CLINME. However, the potential of these new PBR ligands is still under investigation and as a consequence [ C]PK11195 is used so far to image activated microglia cells in neurological disorders. With [ C]PK11195, distinct neuroinflammation was detected in multiple sclerosis, Parkinson ’ s disease, encephalitis and other neurological diseases. Because neuroinflammation plays a central role in the progression of neurodegenerative diseases, anti-inflammatory drugs have been investigated for therapeutic intervention. Especially minocycline and cyclooxygenase inhibitors have shown in vivo anti-inflammatory, hence neuroprotective properties, that could be detected by PET imaging of the PBR with [ C]PK11195. The imaging studies published so far showed that the PBR can be an important target for monitoring disease progression, therapy response and determining the optimal drug dose.
Export Options
About this article
Cite this article as:
Doorduin Janine, de Vries F.J. Erik, Dierckx A. Rudi and Klein C. Hans, PET Imaging of the Peripheral Benzodiazepine Receptor: Monitoring Disease Progression and Therapy Response in Neurodegenerative Disorders, Current Pharmaceutical Design 2008; 14 (31) . https://dx.doi.org/10.2174/138161208786549443
DOI https://dx.doi.org/10.2174/138161208786549443 |
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
-
Neurotoxicity of Insecticides
Current Medicinal Chemistry Role of Nuclear Steroid Receptors in Apoptosis
Current Medicinal Chemistry Spinal Muscular Atrophy: Molecular Mechanisms
Current Molecular Medicine Drp1 in Ischemic Neuronal Death: An Unusual Suspect
Current Medicinal Chemistry Microglial Senescence
CNS & Neurological Disorders - Drug Targets Area, Age and Gender Dependence of the Nucleoside System in the Brain: a Review of Current Literature
Current Topics in Medicinal Chemistry The Neurotrophins and Their Role in Alzheimers Disease
Current Neuropharmacology Therapeutic Approach for Neuronal Disease by Regulating Reninangiotensin System
Current Hypertension Reviews Melatonin, A Natural Programmed Cell Death Inducer in Cancer
Current Medicinal Chemistry Diagnostic and Therapeutic Uses of Nanomaterials in the Brain
Current Medicinal Chemistry Inflammatory Mechanisms and Oxidative Stress as Key Factors Responsible for Progression of Neurodegeneration: Role of Brain Innate Immune System
CNS & Neurological Disorders - Drug Targets Neurotransmitter Effects in Human Immunodeficiency Virus (HIV) and Simian Immuno-Deficiency Virus (SIV) Infection
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Noscapine and its Analogs as Chemotherapeutic Agent: Current updates
Current Topics in Medicinal Chemistry The Protective Effects of Natural Products on Blood-Brain Barrier Breakdown
Current Medicinal Chemistry Erythropoietin and Wnt1 Govern Pathways of mTOR, Apaf-1, and XIAP in Inflammatory Microglia
Current Neurovascular Research Blood-Brain Barrier Transport of Drugs for the Treatment of Brain Diseases
CNS & Neurological Disorders - Drug Targets Ameliorative Effect of Trans-Sinapic Acid and its Protective Role in Cerebral Hypoxia in Aluminium Chloride Induced Dementia of Alzheimer's Type
CNS & Neurological Disorders - Drug Targets Biomarkers in Amyotrophic Lateral Sclerosis: Is There A Neurovascular Pathway?
Current Neurovascular Research Alzheimer’s Disease: New Concepts on the Role of Autoimmunity and NLRP3 Inflammasome in the Pathogenesis of the Disease
Current Neuropharmacology Structural Characterization of Amyloid β17-42 Dimer by Potential of Mean Force Analysis: Insights from Molecular Dynamics Simulations
Protein & Peptide Letters