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Activation of peripheral cannabinoid receptors synergizes the effect of systemic ibuprofen in a pain model in rat

dc.creatorDíaz-Reval, M. Irenees_ES
dc.creatorCárdenas, Yolitzyes_ES
dc.creatorHuerta, Migueles_ES
dc.creatorTrujillo, Xóchitles_ES
dc.creatorSánchez-Pastor, Enrique Alejandroes_ES
dc.creatorGonzález-Trujano, María Evaes_ES
dc.creatorVirgen-Ortíz, Adolfoes_ES
dc.creatorPérez-Hernández, M. Gicelaes_ES
dc.date2022
dc.date.accessioned2024-12-18T19:21:05Z
dc.date.available2024-12-18T19:21:05Z
dc.date.issued2022
dc.identifierJC22NC22es_ES
dc.identifier.urihttp://repositorio.inprf.gob.mx/handle/123456789/8165
dc.identifier.urihttps://doi.org/10.3390/ph15080910
dc.descriptionPharmacological synergism is a current strategy for the treatment of pain. However, few studies have been explored to provide evidence of the possible synergism between a non-steroidal anti-inflammatory drug (NSAID) and a cannabinoid agonist, in order to establish which combinations might be effective to manage pain. The aim of this study was to explore the synergism between ibuprofen (IBU) and the synthetic cannabinoid WIN 55,212-2 (WIN) to improve pain relief by analyzing the degree of participation of the CB1 and CB2 cannabinoid receptors in the possible antinociceptive synergism using an experimental model of pain in Wistar rats. First, the effective dose thirty (ED30) of IBU (10, 40, 80, and 160 mg/kg, subcutaneous) and WIN (3, 10, and 30 µg/p, intraplantar) were evaluated in the formalin test. Then, the constant ratio method was used to calculate the doses of IBU and WIN to be administered in combination (COMB) to determine the possible synergism using the isobolographic method. The participation of the CB1 and CB2 receptors was explored in the presence of the antagonists AM281 and AM630, respectively. The combination of these drugs produced a supra-additive response with an interaction index of 0.13. In addition, AM281 and AM630 antagonists reversed the synergistic effect in 45% and 76%, respectively, suggesting that both cannabinoid receptors are involved in this synergism, with peripheral receptors playing a relevant role. In conclusion, the combination of IBU + WIN synergism is mainly mediated by the participation of the CB2 receptor, which can be a good option for the better management of pain relief.es_ES
dc.formatPDFes_ES
dc.language.isoenges_ES
dc.publisherMDPIes_ES
dc.relation15(8):910
dc.rightsAcceso Cerradoes_ES
dc.titleActivation of peripheral cannabinoid receptors synergizes the effect of systemic ibuprofen in a pain model in rates_ES
dc.typeArtículoes_ES
dc.contributor.affiliationCentro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima 28045, México
dc.contributor.emailidiazre@ucol.mx
dc.relation.jnabreviadoPHARMACEUTICALS
dc.relation.journalPharmaceuticals
dc.identifier.placeSuiza
dc.date.published2022
dc.identifier.organizacionInstituto Nacional de Psiquiatría Ramón de la Fuente Muñiz
dc.identifier.eissn1424-8247
dc.identifier.doi10.3390/ph15080910
dc.subject.kwSynergism
dc.subject.kwAntinociception
dc.subject.kwInflammatory pain
dc.subject.kwFormalin model
dc.subject.kwCannabinoids receptors
dc.subject.kwIbuprofen
dc.subject.kwWIN 55,212-2
dc.subject.kwRats


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