Background: Acute and chronic pain commonly accompany various clinical conditions such as contusion, fracture, osteoarthritis, peripheral neuropathy, and postherpetic neuralgia. Recent studies have found that antioxidative drugs can have analgesic effects. The present study tested the hypothesis that a new anthranilic acid derivative, EAntS-GS, exerts antinociceptive effects on inflammatory pain in a rat model.
Methods: We induced subacute pain with a plantar injection of Freund's complete adjuvant (FCA) in Sprague-Dawley rats. EAntS-GS (1 mg/kg subcutaneous injection or 1% application) was administered every 12 h beginning 24 h after FCA administration, and the plantar test was used to determine its effect on pain. Levels of myeloperoxidase, inducible nitric oxide synthase (iNOS), and protease activated receptor 2 (PAR2) were measured to elucidate the mechanism of action of EAntS-GS.
Results: EAntS-GS significantly reduced FCA-induced pain and myeloperoxidase, iNOS, and PAR2 levels. Our findings suggest that the new anthranilic acid derivative, EAntS-GS, exerts antinociceptive effects, and that the mechanism involves iNOS and PAR2.
Conclusion: We conclude that EAntS-GS should be considered a new therapeutic tool to treat acute and chronic pain.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.jss.2011.03.081 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Targeting Lung Cancer with Carvacrol-Triazole-Arylidenehydrazide Hybrids: In Vitro and In Silico Cytotoxicity Assessments.
Chem Biodivers
January 2025
Bezmialem Vakif University: Bezmialem Vakif Universitesi, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Vatan St., 34093, Istanbul, TURKEY.
In this study, a series of 16 arylidenehydrazide derivatives (7a-7p), hybridized with the natural product carvacrol, were successfully synthesized starting from anthranilic acid methyl ester. The cytotoxic effects of these compounds were examined against two different cell lines, A549 and BEAS-2B. Additionally, in silico studies were conducted to investigate the ligand-protein binding modes and their stabilities.
View Article and Find Full Text PDFGreen one-pot synthesis of quinoxaline derivatives using sulfo-anthranilic acid functionalized alginate-MCFeO nanostructures: a novel superparamagnetic catalyst with antiproliferative potential.
RSC Adv
January 2025
Department of Life Science and Agriculture, Zhoukou Normal University Zhoukou Henan 466001 China
This study reports a green, multi-component synthesis of 2-aminoimidazole-linked quinoxaline Schiff bases using a novel superparamagnetic acid catalyst. The catalyst consists of sulfo-anthranilic acid (SAA) immobilized on MnCoFeO@alginate magnetic nanorods (MNRs), achieving high SAA loading (1.8 mmol g) and product yields (91-97%).
View Article and Find Full Text PDFIdentification of a binding site for small molecule inhibitors targeting human TRPM4.
Nat Commun
January 2025
Laboratory of Biological Electron Microscopy, IPHYS, SB, EPFL, and Dept. Fundamental Microbiology, Faculty of Biology and Medicine, UNIL, Cubotron, Rt. de la Sorge, Lausanne, Switzerland.
Transient receptor potential (TRP) melastatin 4 (TRPM4) protein is a calcium-activated monovalent cation channel associated with various genetic and cardiovascular disorders. The anthranilic acid derivative NBA is a potent and specific TRPM4 inhibitor, but its binding site in TRPM4 has been unknown, although this information is crucial for drug development targeting TRPM4. We determine three cryo-EM structures of full-length human TRPM4 embedded in native lipid nanodiscs without inhibitor, bound to NBA, and an anthranilic acid derivative, IBA.
View Article and Find Full Text PDFDysregulation of the Kynurenine Pathway in Relapsing Remitting Multiple Sclerosis and Its Correlations With Progressive Neurodegeneration.
Neurol Neuroimmunol Neuroinflamm
March 2025
Macquarie Medical School, Faculty of Medicine, Health and Human Sciences, Macquarie University, Sydney.
Background And Objectives: Despite the absence of acute lesion activity in multiple sclerosis (MS), chronic neurodegeneration continues to progress, and a potential underlying mechanism could be the kynurenine pathway (KP). Prolonged activation of the KP from chronic inflammation is known to exacerbate the progression of neurodegenerative diseases through the production of neurotoxic metabolites. Among the 8 KP metabolites, six of them, namely kynurenine (KYN), 3-hydroxylkynurenine (3HK), anthranilic acid (AA), kynurenic acid (KYNA), and quinolinic acid (QUIN), have been associated with neurodegeneration.
View Article and Find Full Text PDFDownregulation and inhibition of TRPM2 calcium channel prevent oxidative stress-induced endothelial dysfunction in the EA.hy926 endothelial cells model - Preliminary studies.
Adv Med Sci
January 2025
Department of Histology and Embryology, Faculty of Medicine, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Toruń, Poland; Faculty of Medicine, Collegium Medicum, Mazovian Academy in Płock, Płock, Poland.
Purpose: Proper functioning of the endothelial barrier is crucial for cardiovascular system homeostasis. Oxidative stress can lead to endothelial dysfunction (ED), damaging lipids, proteins, and DNA. Reactive oxygen species also increase cytoplasmic Ca levels, activating transient receptor potential melastatin 2 (TRPM2), a membrane non-selective calcium channel.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!