Controlling Ca2+ Permeable α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Photochromic Ion Channel Blockers

被引：10
|
作者：
Norager, Niels G. [1 ]
Poulsen, Mette H. [1 ]
Stromgaard, Kristian [1 ]
机构：
[1] Univ Copenhagen, Dept Drug Design & Pharmacol, Univ Pk 2, DK-2100 Copenhagen, Denmark
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2018年 / 61卷 / 17期
关键词：
IONOTROPIC GLUTAMATE RECEPTORS; SOLID-PHASE SYNTHESIS; POLYAMINE TOXINS; CAGED GLUTAMATE; NMDA RECEPTORS; OPTICAL SWITCH; POTENT; OPTOGENETICS; AZOBENZENE; INSIGHTS;
D O I：
10.1021/acs.jmedchem.8b00756
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Ionotropic glutamate receptors (iGluRs) play a critical role in normal brain function and neurodegenerative diseases. Development of light-dependent compounds would enable studies of iGluRs within intact mammalian neural tissue, as light is noninvasive and can be applied with high spatiotemporal precision. Here we develop a potent photochromic antagonist that selectively targets the Ca2+ permeable AMPA-type of iGuRs, thus providing an important tool to study the contribution of AMPA-type iGluRs on neuronal activity.
引用
收藏
页码：8048 / 8053
页数：6
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