Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders.
Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders.
复制标题
DOI：
10.3389/fphar.2018.00030
复制
发表时间：
2018
影响因子：
5.6
通讯作者：
Bhattacharya A
中科院分区：
文献类型：
--
作者：
Bhattacharya A
atp门控P2X7离子通道是CNS中丰富的小胶质蛋白，在执行atp驱动的危险信号转导中起重要的病理作用。新出现的数据引起了科学界对P2X7离子通道作为中枢神经系统疾病潜在药物靶点的兴趣和兴奋。在过去的几年里，关于CNS P2X7生物学的大量数据已经发表，特别是P2X7在小胶质细胞中的作用，以及脑渗透P2X7拮抗剂的体内效应。同样，CNS P2X7配体的药物化学也取得了重大进展，作为CNS疾病模型体内靶点验证的拮抗剂，鉴定了两种临床化合物（JNJ-54175446和JNJ-55308942），最后发现了P2X7 PET配体。这篇综述试图将目前对P2X7在中枢神经系统中的理解与P2X7作为神经精神疾病药物靶点的关注结合起来。
The ATP-gated P2X7 ion channel is an abundant microglial protein in the CNS that plays an important pathological role in executing ATP-driven danger signal transduction. Emerging data has generated scientific interest and excitement around targeting the P2X7 ion channel as a potential drug target for CNS disorders. Over the past years, a wealth of data has been published on CNS P2X7 biology, in particular the role of P2X7 in microglial cells, and in vivo effects of brain-penetrant P2X7 antagonists. Likewise, significant progress has been made around the medicinal chemistry of CNS P2X7 ligands, as antagonists for in vivo target validation in models of CNS diseases, to identification of two clinical compounds (JNJ-54175446 and JNJ-55308942) and finally, discovery of P2X7 PET ligands. This review is an attempt to bring together the current understanding of P2X7 in the CNS with a focus on P2X7 as a drug target in neuropsychiatric disorders.
登录
查看更多内容
影响因子：
3.7
作者：
Feng, Wen-Ping;Zhang, Bo;Liu, Juan
通讯作者：
Liu, Juan
影响因子：
5.1
作者：
Gubert, Carolina;Fries, Gabriel Rodrigo;Oliveira Battastini, Ana Maria
通讯作者：
Oliveira Battastini, Ana Maria
影响因子：
7.3
作者：
Bhattacharya, Anindya;Wang, Qi;Letavic, Michael A.
通讯作者：
Letavic, Michael A.
影响因子：
3.2
作者：
Fantoni ER;Dal Ben D;Falzoni S;Di Virgilio F;Lovestone S;Gee A
通讯作者：
Gee A
影响因子：
5.4
作者：
Backlund, Lena;Nikamo, Pernilla;Osby, Urban
通讯作者：
Osby, Urban