Mechanisms involved in the antinociceptive and anti-inflammatory effects of a new triazole derivative: 5-[1-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl]-1H-tetrazole (LQFM-096)
| Autor: | Dayane Moreira da Silva, Lorrane Kelle da Silva Moreira, Ricardo Menegatti, Fernanda C. A. Santos, Danilo da Silva Lima, Iziara Ferreira Florentino, Daiany P.B. Silva, Luciano M. Lião, Boniek G. Vaz, Elson Alves Costa, José P Vasconcelos, Germán Sanz, James Oluwagbamigbe Fajemiroye, Carina Sofia Cardoso |
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| Rok vydání: | 2019 |
| Předmět: |
0301 basic medicine
Nociception Immunology TRPV1 Anti-Inflammatory Agents Tetrazoles (+)-Naloxone Pharmacology Carrageenan Dinoprostone Glibenclamide 03 medical and health sciences Mice 0302 clinical medicine Oral administration Cell Movement medicine Leukocytes Animals Edema Pharmacology (medical) Pleurisy Pain Measurement Analgesics Chemistry Triazoles 030104 developmental biology Opioid Hyperalgesia Female medicine.symptom Licking 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | Inflammopharmacology. 28(4) |
| ISSN: | 1568-5608 |
| Popis: | The aim of this study was to design, synthesize and evaluate the potential analgesic and anti-inflammatory effects of 5-[1-(4-fluorphenyl)-1H-1,2,3-triazol-4-yl]-1H-tetrazole—(LQFM-096: a new triazole compound) as well as to elucidate its possible mechanisms of action. The oral administration of LQFM-096 (10, 20 or 40 mg/kg) decreased the number of writhing in mice. At the dose of 20 mg/kg, LQFM-096 reduced the licking time at both neurogenic and inflammatory phases of the formalin test. Pretreatment with naloxone (3 mg/kg) and glibenclamide (3 mg/kg) attenuated the antinociceptive effect of LQFM-096 in the first phase of the formalin test. At the dose of 20 mg/kg, LQFM-096 also decreased the licking time in the acidified saline-induced and capsaicin-induced nociception. This effect was blocked by naloxone (3 mg/kg) pretreatment prior to the administration of LQFM-096. In addition, LQFM-096 inhibited hyperalgesia induced by carrageenan and PGE2. Naloxone (3 mg/kg) attenuated the effect of LQFM-096 through disinhibition of PGE2-induced hyperalgesia. The anti-inflammatory effect of LQFM-096 was demonstrated in carrageenan-induced oedema or pleurisy as well as CFA-induced arthritis. The hyperalgesia and cellular migration in CFA-induced arthritis were reduced significantly. Altogether, these findings suggest antinociceptive effect of LQFM-096 and implicate the modulation of ASICs/TRPV1 channels by opioid/KATP pathway. The anti-inflammatory effect of LQFM-096 was mediated by a reduction in oedema, leukocytes migration, TNF-α, PGE2 levels and myeloperoxidase activity. |
| Databáze: | OpenAIRE |
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