The P2X7 receptor is a cation channel activated by high concentrations of adenosine triphosphate (ATP). Upon long-term activation, it complexes with membrane proteins forming a wide pore that leads to cell death and increased release of ATP into the extracellular milieu. The P2X7 receptor is widely expressed in the CNS, such as frontal cortex, hippocampus, amygdala and striatum, regions involved in neurodegenerative diseases and psychiatric disorders. Despite P2X7 receptor functions in glial cells have been extensively studied, the existence and roles of this receptor in neurons are still controversially discussed. Regardless, P2X7 receptors mediate several processes observed in neuropsychiatric disorders and brain tumors, such as activation of neuroinflammatory response, stimulation of glutamate release and neuroplasticity impairment. Moreover, P2X7 receptor gene polymorphisms have been associated to depression, and isoforms of P2X7 receptors are implicated in neuropsychiatric diseases. In view of that, the P2X7 receptor has been proposed to be a potential target for therapeutic intervention in brain diseases. This review discusses the molecular mechanisms underlying P2X7 receptor-mediated signaling in neurodegenerative diseases, psychiatric disorders, and brain tumors. In addition, it highlights the recent advances in the development of P2X7 receptor antagonists that are able of penetrating the central nervous system.

P2X7受体是被高浓度三磷酸腺苷（ATP）激活的阳离子通道。长期激活后，它与膜蛋白复合，形成一个宽孔，导致细胞死亡并增加ATP向细胞外环境的释放。P2X7受体在中枢神经系统中广泛表达，例如额叶皮层，海马，杏仁核和纹状体，涉及神经退行性疾病和精神病的区域。尽管已经广泛研究了神经胶质细胞中P2X7受体的功能，但该受体在神经元中的存在和作用仍存在争议。无论如何，P2X7受体介导在神经精神疾病和脑肿瘤中观察到的多个过程，例如激活神经炎症反应，刺激谷氨酸释放和神经可塑性损害。此外，P2X7受体基因多态性与抑郁症有关，P2X7受体的亚型与神经精神疾病有关。鉴于此，已经提出P2X7受体是脑疾病治疗干预的潜在靶标。这篇综述讨论了神经退行性疾病，精神病和脑肿瘤中P2X7受体介导的信号传导的分子机制。此外，它突显了能够穿透中枢神经系统的P2X7受体拮抗剂的最新进展。这篇综述讨论了神经退行性疾病，精神病和脑肿瘤中P2X7受体介导的信号传导的分子机制。此外，它突显了能够穿透中枢神经系统的P2X7受体拮抗剂的最新进展。这篇综述讨论了神经退行性疾病，精神病和脑肿瘤中P2X7受体介导的信号传导的分子机制。此外，它突出了能够穿透中枢神经系统的P2X7受体拮抗剂的最新进展。