Abstract
Eleven compounds belonging to the chalcone family were tested for their ability to activate and subsequently desensitize the rat transient receptor potential ankyrin 1 cation channel, subfamily A, member 1 (TRPA1) in a heterologous expression system. Four of the tested compounds were more potent than the TRPA1 agonist mustard oil, and showed also a strong desensitizing effect. Some chalcone compounds were not pungent in the eye-wiping assay and quite remarkably inhibited in a long-lasting and dose-dependent manner the pain response in the formalin test. Chalcones can be considered as novel candidates for the development of antihyperalgesic preparations based on TRPA1 desensitization.
Keywords: Chalcones, eye wiping, neuropathic pain, pain, TRPA1.
CNS & Neurological Disorders - Drug Targets
Title:Chalcone Derivatives Activate and Desensitize the Transient Receptor Potential Ankyrin 1 Cation Channel, Subfamily A, Member 1 TRPA1 Ion Channel: Structure-Activity Relationships in vitro and Anti-Nociceptive and Anti-inflammatory Activity in vivo
Volume: 15 Issue: 8
Author(s): Aniello Schiano Moriello, Livio Luongo, Francesca Guida, Michael S. Christodoulou, Dario Perdicchia, Sabatino Maione, Daniele Passarella, Vincenzo Di Marzo and Luciano De Petrocellis
Affiliation:
Keywords: Chalcones, eye wiping, neuropathic pain, pain, TRPA1.
Abstract: Eleven compounds belonging to the chalcone family were tested for their ability to activate and subsequently desensitize the rat transient receptor potential ankyrin 1 cation channel, subfamily A, member 1 (TRPA1) in a heterologous expression system. Four of the tested compounds were more potent than the TRPA1 agonist mustard oil, and showed also a strong desensitizing effect. Some chalcone compounds were not pungent in the eye-wiping assay and quite remarkably inhibited in a long-lasting and dose-dependent manner the pain response in the formalin test. Chalcones can be considered as novel candidates for the development of antihyperalgesic preparations based on TRPA1 desensitization.
Export Options
About this article
Cite this article as:
Moriello Schiano Aniello, Luongo Livio, Guida Francesca, Christodoulou S. Michael, Perdicchia Dario, Maione Sabatino, Passarella Daniele, Marzo Di Vincenzo and Petrocellis De Luciano, Chalcone Derivatives Activate and Desensitize the Transient Receptor Potential Ankyrin 1 Cation Channel, Subfamily A, Member 1 TRPA1 Ion Channel: Structure-Activity Relationships in vitro and Anti-Nociceptive and Anti-inflammatory Activity in vivo, CNS & Neurological Disorders - Drug Targets 2016; 15 (8) . https://dx.doi.org/10.2174/1871527315666160413123621
DOI https://dx.doi.org/10.2174/1871527315666160413123621 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
Call for Papers in Thematic Issues
Diagnosis and treatment of central nervous system infectious diseases
Infectious diseases of the central nervous system (CNS) can be divided into bacterial, tuberculous, viral, fungal, parasitic infections, etc. Early etiological treatment is often the most crucial means to reduce the mortality rate of patients with central nervous system infections, reduce complications and sequelae, and improve prognosis. The initial clinical ...read more
Techniques of Drug Repurposing: Delivering a new life to Herbs & Drugs
Of late, with the adaptation of innovative approaches and integration of advancements made towards medical sciences as well as the availability of a wide range of tools; several therapeutic challenges are being translated into viable clinical solutions, with a high degree of efficacy, safety, and selectivity. With a better understanding ...read more
Trends and perspectives in the rational management of CNS disorders
Central nervous system (CNS) diseases enforce a significant global health burden, driving ongoing efforts to improve our understanding and effectiveness of therapy. This issue investigates current advances in the discipline, focusing on the understanding as well as therapeutic handling of various CNS diseases. The issue covers a variety of diseases, ...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
Related Articles
-
Cell Hierarchy, Metabolic Flexibility and Systems Approaches to Cancer Treatment
Current Pharmaceutical Biotechnology Molecules of Parasites as Immunomodulatory Drugs
Current Topics in Medicinal Chemistry Drugging Cell Cycle Kinases in Cancer Therapy
Current Drug Targets Limiting Functional Deficiency Following Stroke: Exploiting Different Stem Cell Reservoirs
Current Neuropharmacology Editorial [Hot Topic: ErbB Family and Downstream Signal Transduction Pathways as Targets for Anticancer Therapy (Guest Editor: F. Caponigro)]
Current Drug Targets Runx1/AML1 is a Guardian of Hematopoietic Stem Cells
Current Cancer Therapy Reviews Stem Cell Defects in Philadelphia Chromosome Negative Chronic Myeloproliferative Disorders: A Phenotypic and Molecular Puzzle?
Current Stem Cell Research & Therapy Myelodysplastic Syndromes: Review of Pathophysiology and Current Novel Treatment Approaches
Current Cancer Drug Targets When Neighbors Talk: Colon Cancer Cell Invasion and Tumor Microenvironment Myofibroblasts
Current Drug Targets Senescence and Cell Death Pathways and Their Role in Cancer Therapeutic Outcome
Current Medicinal Chemistry The Phosphoinositide 3-Kinase Pathway in Human Cancer: Genetic Alterations and Therapeutic Implications
Current Genomics siRNA-Mediated Knock-Down of P-Glycoprotein Expression Reveals Distinct Cellular Disposition of Anticancer Tyrosine Kinases Inhibitors
Drug Metabolism Letters Molecular Kinetics and Targeting Within the Nucleus
Current Chemical Biology Folate-conjugated Chitosan-poly(ethylenimine) Copolymer As An Efficient and Safe Vector For Gene Delivery in Cancer Cells
Current Gene Therapy Marizomib, a Proteasome Inhibitor for All Seasons: Preclinical Profile and a Framework for Clinical Trials
Current Cancer Drug Targets MicroRNA Regulation of Programmed Cell Death Pathways in Cancer
Current Chemical Biology World Health Organization Classification of Myelodysplastic Syndromes
Current Pharmaceutical Design Folate Based Radiopharmaceuticals for Imaging and Therapy of Cancer and Inflammation
Current Pharmaceutical Design Transcriptomic Effects of Estrogen Starvation and Induction in the MCF7 Cells. The Meta-analysis of Microarray Results
Current Pharmaceutical Biotechnology Bugs as Drugs: Understanding the Linkage between Gut Microbiota and Cancer Treatment
Current Drug Targets