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The P2X7 receptor as a therapeutic target

机译：P2X7受体作为治疗靶标

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Background: The P2X7 receptor is present in a variety of cell types involved in pain, inflammatory processes and neurodegenerative conditions, thus it may be an appealing target for pharmacological intervention. The extensive use of high-throughput screening (HTS) followed by a hit-to-lead (HtL) program, has prompted a number of firms to identify highly selective and metabolically stable small-molecules possessing activity for both the rat and human P2X7 receptor, which provide a novel therapeutic approach to the treatment of pain as well as neurodegenerative and inflammatory disorders. Objective: To describe the current status of and potential for development of P2X7 receptor-antagonists. Methods: A literature review. Results/conclusions: We describe the recent discoveries of novel P2X7 receptor-selective antagonists, along with their biological activity and therapeutic potential.
机译：背景：P2X7受体存在于涉及疼痛，炎症过程和神经退行性疾病的多种细胞类型中，因此它可能是药理干预的引人注目的靶标。高通量筛选（HTS）的广泛使用以及“铅敲击（HtL）”程序的出现，促使许多公司发现对大鼠和人类P2X7受体均具有活性的高选择性和代谢稳定的小分子，它为疼痛以及神经退行性和炎症性疾病的治疗提供了一种新颖的治疗方法。目的：描述P2X7受体拮抗剂的现状和发展潜力。方法：文献复习。结果/结论：我们描述了新型P2X7受体选择性拮抗剂的最新发现，以及它们的生物学活性和治疗潜力。

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