Sigma-1 receptor antagonist (BD-1063) potentiates the antinociceptive effect of quercetin in neuropathic pain induced by chronic constriction injury
Por:
Espinosa-Juárez J.V., Jaramillo-Morales O.A., Déciga-Campos M., Moreno-Rocha L.A., López-Muñoz F.J.
Publicada:
1 ene 2021
Categoría:
Drug discovery
Resumen:
Neuropathic pain is characterized by the presence of hyperalgesia and allodynia. Pharmacological treatments include the use of antiepileptics such as pregabalin or gabapentin, as well as antidepressants; however, given the role of the sigma-1 receptor in the generation and maintenance of pain, it has been suggested that sigma-1 receptor antagonists may be effective. There are also other alternatives that have been explored, such as the use of flavonoids such as quercetin. Due to the relevance of drug combinations in therapeutics, the objective of this work was to evaluate the effect of the combination of BD-1063 with quercetin in a chronic sciatic nerve constriction model using the “Surface of Synergistic Interaction” analysis method. The combination had preferable additive or synergistic effects, with BD-1063 (17.8 mg/kg) + QUER (5.6 mg/kg) showing the best antinociceptive effects. The required doses were also lower than those used individually to obtain the same level of effect. Our results provide the first evidence that the combination of a sigma-1 receptor antagonist and the flavonoid quercetin may be useful in the treatment of nociceptive behaviors associated with neuropathic pain, suggesting a new therapeutic alternative for this type of pain. © 2020 Wiley Periodicals LLC
Filiaciones:
Espinosa-Juárez J.V.:
Escuela de Ciencias Químicas sede Ocozocoautla, Universidad Autónoma de Chiapas, Ocozocoautla de Espinosa, Chiapas, Mexico
Jaramillo-Morales O.A.:
Departamento de Enfermería y Obstetricia. División de Ciencias de la Vida, Campus Irapuato-Salamanca, Universidad de Guanajuato. Carretera Irapuato-Silao km. 9, El copal, complejo 2 de la DICIVA, Irapuato, Guanajuato, Mexico
Déciga-Campos M.:
Sección de Estudios de Posgrado e Investigación de la Escuela Superior de Medicina, Instituto Politécnico Nacional, Ciudad de México, Mexico
Moreno-Rocha L.A.:
Departamento Sistemas Biológicos, Universidad Autónoma Metropolitana, Unidad Xochimilco, México City, Mexico
López-Muñoz F.J.:
Departamento de Farmacobiología, CINVESTAV-Sede Sur, Ciudad de México, Mexico
|