神经胶质细胞激活在神经病理性疼痛(NP)发生和维持中发挥重要作用.Toll样受体4(TLR4)通过激活中枢神经系统胶质细胞(主要是小胶质细胞),诱导促炎因子、神经活性物质等的释放,参与NP的形成和维持及阿片类药物的不良反应,已成为潜在的NP治疗靶标.靶向抑制TLR4的生物学效应在NP模型中已取得初步疗效,其中TLR4信号通路抑制剂-异丁司特已进入Ⅱ期临床试验.本文主要综述TLR4的结构、功能、作用机制、靶向药物研发现状等.%Activation of microglia plays a vital role in the initiation and maintenance of specific neuropathic pain states. By activating microglia in central nervous system, Toll-like receptor 4 (TLR4) can promote the release of proinflammatory cytokines and neuroactive compounds, participate in the initiation and maintenance of neuropathic pain, and trigger the opiate side effects. Therefore, TLR4 may be a potential therapeutic target for neuropathic pain. Inhibition of TLR4 has shown some biological effects in neuropathic pain models and ibudilast (the TLR4 pathway-inhibiting agent) has been approved for for phase II clinical trials. This article briefly reviews the structure, function, and mechanism of TLR4 as well as the development of TLR4-targeted drugs.
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