Abstract
In the late 1990s, a series of experiments carried out independently in two laboratories led to establish an important connection between the function of the endocannabinoids, which, as exemplified in this special issue, is per se very complex and ubiquitous in animals, and that of the transient receptor potential (TRP) channels, a large family of plasma membrane cation channels involved in several mammalian and non-mammalian physiological and pathological conditions, overlapping only in part with those in which the cannabinoid receptors participate. These experiments were initially based on the observation that the endocannabinoid anandamide and the xenobiotic ligand of TRP channels of V1 type (TRPV1), capsaicin, are somehow chemically similar, both compounds being fatty acid amides, as are also synthetic activators of these channels and inhibitors of anandamide cellular re-uptake. As discussed in this article, the same type of “chemical thoughts” led to the discovery of N-arachidonoyl-dopamine, an endogenous ligand of TRPV1 channels that behaves also an endocannabinoid. The overlap between the ligand recognition properties of some TRP channels and proteins of the endocannabinoid system, namely the cannabinoid receptors and the proteins and enzymes catalyzing anandamide cellular re-uptake and hydrolysis, is being actively explored through the rational design and synthesis of new endocannabinoid- based drugs with multiple mechanisms of action. These aspects are discussed in this review article, together with the possible functional and pharmacological consequences of endocannabinoid-TRP channel interactions.
Keywords: Endocannabinoids, TRPV1, TRPA1, TRPM8
Current Medicinal Chemistry
Title: Endocannabinoids as Regulators of Transient Receptor Potential (TRP)Channels: a Further Opportunity to Develop New Endocannabinoid-Based Therapeutic Drugs
Volume: 17 Issue: 14
Author(s): V. Di Marzo and L. De Petrocellis
Affiliation:
Keywords: Endocannabinoids, TRPV1, TRPA1, TRPM8
Abstract: In the late 1990s, a series of experiments carried out independently in two laboratories led to establish an important connection between the function of the endocannabinoids, which, as exemplified in this special issue, is per se very complex and ubiquitous in animals, and that of the transient receptor potential (TRP) channels, a large family of plasma membrane cation channels involved in several mammalian and non-mammalian physiological and pathological conditions, overlapping only in part with those in which the cannabinoid receptors participate. These experiments were initially based on the observation that the endocannabinoid anandamide and the xenobiotic ligand of TRP channels of V1 type (TRPV1), capsaicin, are somehow chemically similar, both compounds being fatty acid amides, as are also synthetic activators of these channels and inhibitors of anandamide cellular re-uptake. As discussed in this article, the same type of “chemical thoughts” led to the discovery of N-arachidonoyl-dopamine, an endogenous ligand of TRPV1 channels that behaves also an endocannabinoid. The overlap between the ligand recognition properties of some TRP channels and proteins of the endocannabinoid system, namely the cannabinoid receptors and the proteins and enzymes catalyzing anandamide cellular re-uptake and hydrolysis, is being actively explored through the rational design and synthesis of new endocannabinoid- based drugs with multiple mechanisms of action. These aspects are discussed in this review article, together with the possible functional and pharmacological consequences of endocannabinoid-TRP channel interactions.
Export Options
About this article
Cite this article as:
Marzo Di V. and Petrocellis De L., Endocannabinoids as Regulators of Transient Receptor Potential (TRP)Channels: a Further Opportunity to Develop New Endocannabinoid-Based Therapeutic Drugs, Current Medicinal Chemistry 2010; 17 (14) . https://dx.doi.org/10.2174/092986710790980078
DOI https://dx.doi.org/10.2174/092986710790980078 |
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
-
Human Sirtuins: An Overview of an Emerging Drug Target in Age-Related Diseases and Cancer
Current Drug Targets Meloxicam Prevents Load-Induced Cardiac Hypertrophy in Mice
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Targeting p73 - a Potential Approach in Cancer Treatment
Current Pharmaceutical Design Upregulation of Focal Adhesion Kinase by 14-3-3ε via NFκB Activation in Hepatocellular Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Cellular and Biochemical Actions of Melatonin which Protect Against Free Radicals: Role in Neurodegenerative Disorders
Current Neuropharmacology New Improved Drug Delivery Technologies for Pentacyclic Triterpenes: A Review
Protein & Peptide Letters Molecular Mechanisms, Biological Actions, and Neuropharmacology of the Growth-Associated Protein GAP-43
Current Neuropharmacology Possibility of Non-Immunosuppressive Immunophilin Ligands as Potential Therapeutic Agents for Parkinsons Disease
Current Pharmaceutical Design Patents Related to Cancer Stem Cell Research
Recent Patents on DNA & Gene Sequences Opiate Drug Use and the Pathophysiology of NeuroAIDS
Current HIV Research Hippocampal BDNF Expression in a Tau Transgenic Mouse Model
Current Alzheimer Research Histopathological Determinants of Tumor Resistance: A Special Look to the Immunohistochemical Expression of Carbonic Anhydrase IX in Human Cancers
Current Medicinal Chemistry Activation of Sphingosine Kinase-1 in Cancer: Implications for Therapeutic Targeting
Current Molecular Pharmacology Marine Peptides and Related Compounds in Clinical Trial+
Anti-Cancer Agents in Medicinal Chemistry Mechanism of Action of Limonene in Tumor Cells: A Systematic Review and Meta-Analysis
Current Pharmaceutical Design Protein Aggregation in Alzheimers Disease and Other Neoropathological Disorders
Current Alzheimer Research In silico Studies Toward the Discovery of Novel Type-II Inhibitors of TrkA: Pharmacophore-based 3D-QSAR Modeling, Database Screening and Molecular Docking
Letters in Drug Design & Discovery Altered Arginine Metabolism in Cells Transfected with Human Wild-Type Beta Amyloid Precursor Protein (βAPP)
Current Alzheimer Research Cellular Uptake and Organ Accumulation of Amphipolar Metallocorroles with Cytoprotective and Cytotoxic Properties
Anti-Cancer Agents in Medicinal Chemistry The Neurotrophins and Their Role in Alzheimers Disease
Current Neuropharmacology