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

页码：8048 / 8053

页数：6

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