Abstract
AMPA receptors mediate fast excitatory synaptic transmission and are essential for synaptic plasticity. ANQX, a photoreactive AMPA receptor antagonist, is an important biological probe used to irreversibly inactivate AMPA receptors. Here, using X-ray crystallography and mass spectroscopy, we report that ANQX forms two major products in the presence of the GluR2 AMPAR ligand-binding core (S1S2J). Upon photostimulation, ANQX reacts intramolecularly to form FQX or intermolecularly to form a covalent adduct with Glu705.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Binding Sites
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Crystallography, X-Ray
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Excitatory Amino Acid Antagonists / chemistry
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Excitatory Amino Acid Antagonists / pharmacology*
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Mass Spectrometry
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Models, Molecular
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Molecular Structure
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Nitro Compounds / chemistry
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Nitro Compounds / pharmacology*
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Quinolines / chemistry
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Quinolines / pharmacology*
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Receptors, AMPA / antagonists & inhibitors*
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Receptors, AMPA / chemistry
Substances
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6-azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione
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Excitatory Amino Acid Antagonists
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Nitro Compounds
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Quinolines
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Receptors, AMPA