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Review Article

嘌呤能P2X7受体拮抗剂的构效关系及治疗潜力

卷 31, 期 11, 2024

发表于: 26 May, 2023

页: [1361 - 1403] 页: 43

弟呕挨: 10.2174/0929867330666230403094538

价格: $65

摘要

嘌呤能P2X7受体(P2X7R)是一种atp门控的非选择性阳离子通道，已成为炎症的守门人，控制促炎细胞因子的释放。作为启动炎症信号级联的关键角色，P2X7受体目前正受到密切关注，作为治疗不同病理的靶点，包括慢性炎症性疾病(类风湿关节炎和骨关节炎)、慢性神经性疼痛、情绪障碍(抑郁和焦虑)、神经退行性疾病、缺血、癌症(白血病)等。由于这些原因，制药公司已经投资于发现能够调节P2X7R的化合物，并提交了许多专利申请。本文综述了P2X7R的结构、功能和组织分布，重点介绍了P2X7R在炎症中的作用。接下来，我们通过强调其作为治疗炎症性疾病和神经退行性疾病的临床候选药物的特性和品质，说明了不同化学类别的非竞争性P2X7R拮抗剂的报道。我们还讨论了开发有效的正电子发射断层扫描(PET)放射配体的努力，以推进对神经退行性疾病病理机制的理解，提供药物靶点结合的证据，并协助临床剂量选择新的药物治疗方法。

关键词: 嘌呤能P2X7受体，炎症，拮抗剂，神经退行性疾病，癌症，自身免疫性疾病，正电子发射断层扫描。

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