Abstract
The cannabinoid CB1 and CB2 receptors are Class A G protein-coupled receptors (GPCRs). While many Class A GPCRs have endogenous ligands that are hydrophilic cations (e.g., the serotonin and dopamine receptors), the cannabinoid receptors have neutral, highly lipophilic ligands derived from the fatty acid, arachidonic acid. The most well-studied of these are N-arachidonoylethanolamine (anandamide, AEA) and sn-2-arachidonoylglycerol (2-AG). This review focuses on the experimental and computational studies that have been used to probe the nature of endocannabinoid interaction with the cannabinoid receptors. These studies include mutation, SAR and NMR studies, as well as, QSAR, docking and molecular dynamics simulations. Gaps in our knowledge are identified. The review begins more generally, however, by discussing the entire endocannabinoid system, of which the cannabinoid receptors are part. For in order to understand endocannabinoid action, one needs an appreciation for the environments for which these ligands have been designed and the conformational changes these ligands must undergo in order to act on the cannabinoid receptors.
Keywords: Cannabinoid, GPCR, endocannabinoid, anandamide, 2-AG, molecular dynamics, QSAR, mutation
Current Medicinal Chemistry
Title: Endocannabinoid Binding to the Cannabinoid Receptors: What Is Known and What Remains Unknown
Volume: 17 Issue: 14
Author(s): Patricia H. Reggio
Affiliation:
Keywords: Cannabinoid, GPCR, endocannabinoid, anandamide, 2-AG, molecular dynamics, QSAR, mutation
Abstract: The cannabinoid CB1 and CB2 receptors are Class A G protein-coupled receptors (GPCRs). While many Class A GPCRs have endogenous ligands that are hydrophilic cations (e.g., the serotonin and dopamine receptors), the cannabinoid receptors have neutral, highly lipophilic ligands derived from the fatty acid, arachidonic acid. The most well-studied of these are N-arachidonoylethanolamine (anandamide, AEA) and sn-2-arachidonoylglycerol (2-AG). This review focuses on the experimental and computational studies that have been used to probe the nature of endocannabinoid interaction with the cannabinoid receptors. These studies include mutation, SAR and NMR studies, as well as, QSAR, docking and molecular dynamics simulations. Gaps in our knowledge are identified. The review begins more generally, however, by discussing the entire endocannabinoid system, of which the cannabinoid receptors are part. For in order to understand endocannabinoid action, one needs an appreciation for the environments for which these ligands have been designed and the conformational changes these ligands must undergo in order to act on the cannabinoid receptors.
Export Options
About this article
Cite this article as:
Reggio H. Patricia, Endocannabinoid Binding to the Cannabinoid Receptors: What Is Known and What Remains Unknown, Current Medicinal Chemistry 2010; 17 (14) . https://dx.doi.org/10.2174/092986710790980005
DOI https://dx.doi.org/10.2174/092986710790980005 |
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
-
Deubiquitinating Enzyme Inhibitors and their Potential in Cancer Therapy
Current Cancer Drug Targets Anaplastic Lymphoma Kinase as a Therapeutic Target in Anaplastic Large Cell Lymphoma, Non-Small Cell Lung Cancer and Neuroblastoma
Anti-Cancer Agents in Medicinal Chemistry Natural Proteinaceous Inhibitors of Serine Proteases
Current Pharmaceutical Design Adenosine A1 Receptor: Analysis of the Potential Therapeutic Effects Obtained by its Activation in the Central Nervous System
Current Medicinal Chemistry Computational Studies Applied to Anti-inflammatory Drug Discovery: A Review
Current Organic Chemistry New Generation of Nitrite Functionalized Star-like Polyvinyl Imidazolium Compound: Application as a Nitrosonium Source and Three Dimensional Nanocatalyst for the Synthesis of Azo Dyes
Letters in Organic Chemistry Heterodimeric Amino Acid Transporters: Molecular Biology and Pathological and Pharmacological Relevance
Current Drug Metabolism The Impact of Crystallographic Data for the Development of Machine Learning Models to Predict Protein-Ligand Binding Affinity
Current Medicinal Chemistry Recent Progress on the Role of Fibronectin in Tumor Stromal Immunity and Immunotherapy
Current Topics in Medicinal Chemistry Structural Comparison of p38 Inhibitor-Protein Complexes: A Review of Recent p38 Inhibitors Having Unique Binding Interactions
Current Topics in Medicinal Chemistry <i>In silico</i> Molecular Docking of SARS-CoV-2 Surface Proteins with Benzimidazole Scaffolds: Strategy to Discover Lead Compounds
Coronaviruses Immunity Modulators, Repurposed Drugs and Candidate Vaccines for COVID-19: A Review
Coronaviruses The Development of HEPT-Type HIV Non-Nucleoside Reverse Transcriptase Inhibitors and Its Implications for DABO Family
Current Pharmaceutical Design Medicinal and Therapeutic Potential of Herbs and Plant Metabolites / Extracts Countering Viral Pathogens - Current Knowledge and Future Prospects
Current Drug Metabolism Synthesis, Characterization, and Antibacterial Properties of ZnO Nanostructures Functionalized Flexible Carbon Fibers
Recent Patents on Nanotechnology Automated Parallel Solid-Phase Synthesis of Non-Peptide CCR1 Receptor Antagonists
Combinatorial Chemistry & High Throughput Screening Synthesis of 1,1-Dioxobenzo[b]thiophene-2-ylmethyloxycarbonyl (Bsmoc) Protected N-Methyl Amino Acids by Reduction of Bsmoc-5-Oxazolidinones and Their Use in Peptide Synthesis
Protein & Peptide Letters Recent Patents Regarding Essential Oils and the Significance of their Constituents in Human Health and Treatment
Recent Patents on Anti-Infective Drug Discovery Biomarkers and Osteosarcoma and IGF
Recent Patents on Biomarkers Effects of Alcohol in the Lung
Current Respiratory Medicine Reviews