P2X3 monomeric receptors (P2X3Rs) and P2X2/3 heteromeric receptors (P2X2/3Rs) in primary sensory neurons and microglial P2X4 monomeric receptors (P2X4Rs) in the spinal dorsal horn (SDH) play important roles in neuropathic pain. In particular, P2X4R in the spinal microglia during peripheral nerve injury (PNI), experimental autoimmune neuritis, and herpes models are useful to explore the potential strategies for developing new drugs to treat neuropathic pain. Recently, novel P2X4 antagonists, NP-1815-PX and NC-2600, were developed, which demonstrated potent and specific inhibition against rodent and human P2X4Rs. The phase I study of NC-2600 has been completed, and no serious side effects were reported. The roles played by purinergic receptors in evoking neuropathic pain provide crucial insights into the pathogenesis of neuropathic pain.

初级感觉神经元中的 P2X3 单体受体 (P2X3Rs) 和 P2X2/3 异聚体受体 (P2X2/3Rs) 和脊髓背角 (SDH) 中的小胶质细胞 P2X4 单体受体 (P2X4Rs) 在神经性疼痛中起重要作用。特别是，周围神经损伤 (PNI)、实验性自身免疫性神经炎和疱疹模型期间脊髓小胶质细胞中的 P2X4R 有助于探索开发治疗神经性疼痛的新药的潜在策略。最近，开发了新型 P2X4 拮抗剂 NP-1815-PX 和 NC-2600，它们显示出对啮齿动物和人类 P2X4R 的有效和特异性抑制。NC-2600 的 I 期研究已经完成，没有报告严重的副作用。嘌呤能受体在诱发神经性疼痛中的作用为神经性疼痛的发病机制提供了重要的见解。