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Review Article

P2受体拮抗剂的潜在治疗应用：从实验室到临床试验

卷 20, 期 9, 2019

页: [919 - 937] 页: 19

弟呕挨: 10.2174/1389450120666190213095923

价格: $65

摘要

背景：细胞外嘌呤和嘧啶在哺乳动物中具有重要的生理功能。嘌呤和嘧啶作用于P1和P2嘌呤能受体，其在各种细胞类型的质膜中广泛表达。 P2受体作为重要的治疗靶标并且与几种病症相关，例如疼痛，神经变性，癌症，炎症和血栓形成。然而，除P2Y12外，临床治疗中P2受体拮抗剂的使用是一项巨大的挑战。目前，许多研究小组和制药公司正致力于开发针对每种受体亚型的特异性拮抗剂分子，其可用作治疗其各自疾病的新药。 目的：本综述汇总了P2受体拮抗剂在不同体外和体内实验模型中的应用以及这些化合物的高级临床试验进展的一些有趣发现。 结论：尽管在实验室中获得了所有令人兴奋的结果，但很少有P2受体拮抗剂进入临床试验，一旦达到这一阶段，治疗的有效性就不能得到保证，如P2X7拮抗剂的例子。尽管如此，P2Y12受体拮抗剂已有成功的历史，并已用于治疗至少二十年，以预防有心肌梗塞风险的患者的血栓形成。这一突破是科学家开发出对其他P2受体具有拮抗活性的新药的动机;因此，在几年内，我们将在嘌呤能治疗领域取得进展。

关键词: P2X受体，P2Y受体，拮抗剂，治疗，血栓形成，疼痛，炎症，临床试验。

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