Abstract
During the last years the development of approaches to multitarget drug design and discovery is gaining acceptance. The cannabinoids are potentially excellent multi-target drug candidates because of their interesting pharmacological profiles, among which stands out the dual capacity of cannabinoid ligands to act as cannabinoid agonist and cholinesterase inhibitors. In this article, inhibition, kinetics studies and docking simulations with a representative set of cannabinoids are presented. The results of these studies showed the inhibitory capacity of some agonist cannabinoids with selectivity at AChE or BuChE enzymes. The kinetic and modelling studies allowed us to postulate the potential mode of action and the binding site of the cannabinoids. In general, the studied cannabinoids showed a mixed type inhibition mode of action. The exception to this behaviour was found for the agonist CP-55,940 that showed a non-competitive inhibition, suggesting that this cannabinoid only binds to the peripheral site.
Keywords: Alzheimer disease, agonist cannabinoids, cholinesterase inhibitors, multitarget drugs
Current Alzheimer Research
Title:Multitarget Cannabinoids as Novel Strategy for Alzheimer Disease
Volume: 10 Issue: 3
Author(s): Pedro Gonzalez-Naranjo, Nuria E. Campillo, Concepcion Perez and Juan A. Paez
Affiliation:
Keywords: Alzheimer disease, agonist cannabinoids, cholinesterase inhibitors, multitarget drugs
Abstract: During the last years the development of approaches to multitarget drug design and discovery is gaining acceptance. The cannabinoids are potentially excellent multi-target drug candidates because of their interesting pharmacological profiles, among which stands out the dual capacity of cannabinoid ligands to act as cannabinoid agonist and cholinesterase inhibitors. In this article, inhibition, kinetics studies and docking simulations with a representative set of cannabinoids are presented. The results of these studies showed the inhibitory capacity of some agonist cannabinoids with selectivity at AChE or BuChE enzymes. The kinetic and modelling studies allowed us to postulate the potential mode of action and the binding site of the cannabinoids. In general, the studied cannabinoids showed a mixed type inhibition mode of action. The exception to this behaviour was found for the agonist CP-55,940 that showed a non-competitive inhibition, suggesting that this cannabinoid only binds to the peripheral site.
Export Options
About this article
Cite this article as:
Gonzalez-Naranjo Pedro, E. Campillo Nuria, Perez Concepcion and A. Paez Juan, Multitarget Cannabinoids as Novel Strategy for Alzheimer Disease, Current Alzheimer Research 2013; 10 (3) . https://dx.doi.org/10.2174/1567205011310030002
DOI https://dx.doi.org/10.2174/1567205011310030002 |
Print ISSN 1567-2050 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5828 |
Call for Papers in Thematic Issues
New Advances in the Prevention, Diagnosis, Treatment, and Rehabilitation of Alzheimer's Disease
Aims and Scope: Introduction: Alzheimer's disease (AD) poses a significant global health challenge, with an increasing prevalence that demands concerted efforts to advance our understanding and strategies for prevention, diagnosis, treatment, and rehabilitation. This thematic issue aims to bring together cutting-edge research and innovative approaches from multidisciplinary perspectives to address ...read more
Current updates on the Role of Neuroinflammation in Neurodegenerative Disorders
Neuroinflammation is an invariable hallmark of chronic and acute neurodegenerative disorders and has long been considered a potential drug target for Alzheimer?s disease (AD) and dementia. Significant evidence of inflammatory processes as a feature of AD is provided by the presence of inflammatory markers in plasma, CSF and postmortem brain ...read more
Deep Learning for Advancing Alzheimer's Disease Research
Alzheimer's disease (AD) poses a significant global health challenge, with an increasing number of individuals affected yearly. Deep learning, a subfield of artificial intelligence, has shown immense potential in various domains, including healthcare. This thematic issue of Current Alzheimer Research explores the application of deep learning techniques in advancing our ...read more
Diagnostic and therapeutic biomarkers of dementia
Dementia affects 18 million people worldwide. Dementia is a syndrome of symptoms caused by brain disease, usually chronic or progressive, clinically characterized by multiple impairments of higher cortical functions such as memory, thinking, orientation, and learning. In addition, in the course of dementia, cognitive deficits are observed, which often hinder ...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
-
Poor Nutrition with Aging: an “Oxidatively Stressing” Condition
Current Nutrition & Food Science Circadian Cycle and Chronotherapeutics: Recent Trend for the Treatment of Various Biological Disorders
Recent Patents on Drug Delivery & Formulation β-Amyloid, Neuronal Death and Alzheimers Disease
Current Molecular Medicine Diabetic CVD – Focus on Vitamin D
Cardiovascular & Hematological Agents in Medicinal Chemistry Aporphines and Parkinson’s Disease: Medical Tools for the Future
Current Topics in Medicinal Chemistry Molecular Targets in the Rational Design of AD Specific PET Tracers: Tau or Amyloid Aggregates?
Current Alzheimer Research Sleep Apnea and Coronary Heart Disease: From Dusk Till Dawn and Further
Current Respiratory Medicine Reviews Neurodegenerative Diseases of the Retina and Potential for Protection and Recovery
Current Neuropharmacology Neovascular Age-Related Macular Degeneration and its Association with Alzheimer’s Disease
Current Aging Science Metabolic Profiling in Multiple Sclerosis and Other Disorders by Quantitative Analysis of Cerebrospinal Fluid Using Nuclear Magnetic Resonance Spectroscopy
Current Pharmaceutical Biotechnology The Mammalian Tachykinin Ligand-Receptor System: An Emerging Target for Central Neurological Disorders
CNS & Neurological Disorders - Drug Targets Non-steroidal Anti-inflammatory Drugs and Cyclooxygenase in Alzheimer s Disease
Current Drug Targets The Role of Adipocytokines in Atherogenesis and Atheroprogression
Current Drug Targets Effect of Antipsychotic Drugs on Cerebrovascular Morbidity and Mortality: A Systematic Review
Current Drug Therapy Evolution of Antipsychotic Intervention in the Schizophrenic Psychosis
Current Drug Targets Plasma Clusterin Levels and the rs11136000 Genotype in Individuals with Mild Cognitive Impairment and Alzheimer’s Disease
Current Alzheimer Research Obesity and Cardiovascular Physiology: Impact of some Pharmacological Agents
Current Vascular Pharmacology Preface
Current Enzyme Inhibition Biotechnological Approaches for the Treatment of Inflammatory Diseases
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Disease State, Age, Sex, and Post-Mortem Time-Dependent Expression of Proteins in AD vs. Control Frontal Cortex Brain Samples
Current Alzheimer Research