• Mol Pain · Jan 2022

    P2X7 receptor induces microglia polarization to the M1 phenotype in cancer-induced bone pain rat models.

    • Ping Wu, Guohua Zhou, Xiaoqi Wu, Run Lv, Jiaqi Yao, and Qingping Wen.
    • Department of Anesthesiology, 74710The First Affiliated Hospital of Dalian Medical University, Dalian, China.
    • Mol Pain. 2022 Jan 1; 18: 17448069211060962.

    BackgroundThe transition from pro-inflammatory M1 phenotype to anti-inflammatory M2 phenotype presents a novel therapeutic strategy for chronic pain.ObjectiveWe investigated the role of microglia polarization in cancer-induced bone pain (CIBP), as well as the role of the P2X7 receptor in modulating M1 to M2 polarization.MethodsWalker-256 breast cancer cells were administered into tibias of female rats to induce bone cancer-associated cancer.ResultsDuring bone cancer development, the P2X7 receptor and M1 microglia markers were upregulated. In contrast, inhibition of the P2X7 receptor by BBG, a blood-brain barrier-permeable P2X7R-specific antagonist, alleviated the pain and promoted microglia polarization toward the M2 phenotype, while suppressing the M1 phenotype in vivo and in vitro.ConclusionP2X7 receptor-mediated spinal microglia polarization is involved in alleviation of CIBP. Therefore, P2X7R is a potential option for CIBP treatment.

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