TY - JOUR
T1 - Sigma-1 receptor antagonist (BD-1063) potentiates the antinociceptive effect of quercetin in neuropathic pain induced by chronic constriction injury
AU - Espinosa-Juárez, Josué Vidal
AU - Jaramillo-Morales, Osmar Antonio
AU - Déciga-Campos, Myrna
AU - Moreno-Rocha, Luis Alfonso
AU - López-Muñoz, Francisco Javier
N1 - Publisher Copyright:
© 2020 Wiley Periodicals LLC
PY - 2021/4
Y1 - 2021/4
N2 - 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.
AB - 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.
KW - BD-1063
KW - neuropathic pain
KW - pain
KW - quercetin
KW - synergism
UR - http://www.scopus.com/inward/record.url?scp=85092353771&partnerID=8YFLogxK
U2 - 10.1002/ddr.21750
DO - 10.1002/ddr.21750
M3 - Artículo
C2 - 33051885
AN - SCOPUS:85092353771
SN - 0272-4391
VL - 82
SP - 267
EP - 277
JO - Drug Development Research
JF - Drug Development Research
IS - 2
ER -