炎症
疾病
免疫系统
神经科学
促炎细胞因子
受体
生物
门控
基因剔除小鼠
医学
免疫学
生物信息学
内科学
作者
Rachael Bartlett,Leanne Stokes,Ronald Sluyter
出处
期刊:Pharmacological Reviews
[American Society for Pharmacology & Experimental Therapeutics]
日期:2014-06-13
卷期号:66 (3): 638-675
被引量:349
标识
DOI:10.1124/pr.113.008003
摘要
The P2X7 receptor is a trimeric ATP-gated cation channel found predominantly, but not exclusively, on immune cells. P2X7 activation results in a number of downstream events, including the release of proinflammatory mediators and cell death and proliferation. As such, P2X7 plays important roles in various inflammatory, immune, neurologic and musculoskeletal disorders. This review focuses on the use of P2X7 antagonists in rodent models of neurologic disease and injury, inflammation, and musculoskeletal and other disorders. The cloning and characterization of human, rat, mouse, guinea pig, dog, and Rhesus macaque P2X7, as well as recent observations regarding the gating and permeability of P2X7, are discussed. Furthermore, this review discusses polymorphic and splice variants of P2X7, as well as the generation and use of P2X7 knockout mice. Recent evidence for emerging signaling pathways downstream of P2X7 activation and the growing list of negative and positive modulators of P2X7 activation and expression are also described. In addition, the use of P2X7 antagonists in numerous rodent models of disease is extensively summarized. Finally, the use of P2X7 antagonists in clinical trials in humans and future directions exploring P2X7 as a therapeutic target are described.
科研通智能强力驱动
Strongly Powered by AbleSci AI