4.7 Article

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

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 61, Issue 17, Pages 8048-8053

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.8b00756

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Funding

  1. GluTarget (University of Copenhagen)

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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.

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