Antinociceptive effects of new pyrazoles compounds mediated by the ASIC-1α channel, TRPV-1 and μMOR receptors.
Acid Sensing Ion Channels
/ metabolism
Action Potentials
/ drug effects
Analgesics
/ chemistry
Animals
Male
Mice
Molecular Structure
Nociception
/ drug effects
Oocytes
/ drug effects
Pain Measurement
Patch-Clamp Techniques
Pyrazoles
/ chemistry
Receptors, Opioid, mu
/ metabolism
TRPV Cation Channels
/ metabolism
Xenopus laevis
Analgesic
Electrophysiology
Ion channels
Pain
Pyrazole compounds
Receptor
Xenopus laevis
Journal
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
ISSN: 1950-6007
Titre abrégé: Biomed Pharmacother
Pays: France
ID NLM: 8213295
Informations de publication
Date de publication:
Jul 2019
Jul 2019
Historique:
received:
26
10
2018
revised:
23
04
2019
accepted:
23
04
2019
pubmed:
6
5
2019
medline:
15
1
2020
entrez:
6
5
2019
Statut:
ppublish
Résumé
Pyrazoles are potent medicinal scaffolds and exhibit a wide spectrum of biological activities, such as analgesic, anti-inflammatory and antipyretic. In this paper we report on research we have performed with the aim of continuing the biological evaluation of the regio-isomeric pyrazole compounds, LQFM-020 (fluorine, para position), LQFM-021 (fluorine, meta position), and LQFM-039 (fluorine, ortho position) in models of pain induced by acidified saline, capsaicin, and formalin. We also investigated the mechanisms of action of these compounds via electrophysiological analyses using the two-electrode voltage-clamp technique and heterologous expression in Xenopus laevis oocytes. This enabled us to study different potassium channel subtypes: the ASIC-1α channel, TRPV-1, and μMOR receptors. Our results indicate that LQFM-020, LQFM-021, and LQFM-039 (15, 30 or 60 mg.kg
Identifiants
pubmed: 31055237
pii: S0753-3322(18)37635-2
doi: 10.1016/j.biopha.2019.108915
pii:
doi:
Substances chimiques
ASIC1 protein, mouse
0
Acid Sensing Ion Channels
0
Analgesics
0
Pyrazoles
0
Receptors, Opioid, mu
0
TRPV Cation Channels
0
TRPV1 protein, mouse
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
108915Informations de copyright
Copyright © 2019 The Authors. Published by Elsevier Masson SAS.. All rights reserved.