Issue 1, 2017

Optical control of AMPA receptors using a photoswitchable quinoxaline-2,3-dione antagonist

Abstract

AMPA receptors respond to the neurotransmitter glutamate and play a critical role in excitatory neurotransmission. They have been implicated in several psychiatric disorders and have rich pharmacology. Antagonists of AMPA receptors have been explored as drugs and one has even reached the clinic. We now introduce a freely diffusible photoswitchable antagonist that is selective for AMPA receptors and endows them with light-sensitivity. Our photoswitch, ShuBQX-3, is active in its dark-adapted trans-isoform but is significantly less active as its cis-isoform. ShuBQX-3 exhibits a remarkable red-shifting of its photoswitching properties through interactions with the AMPA receptor ligand binding site. Since it can be used to control action potential firing with light, it could emerge as a powerful tool for studying synaptic transmission with high spatial and temporal precision.

Graphical abstract: Optical control of AMPA receptors using a photoswitchable quinoxaline-2,3-dione antagonist

Supplementary files

Article information

Article type
Edge Article
Submitted
12 Apr 2016
Accepted
01 Aug 2016
First published
24 Aug 2016
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY license

Chem. Sci., 2017,8, 611-615

Optical control of AMPA receptors using a photoswitchable quinoxaline-2,3-dione antagonist

D. M. Barber, S. Liu, K. Gottschling, M. Sumser, M. Hollmann and D. Trauner, Chem. Sci., 2017, 8, 611 DOI: 10.1039/C6SC01621A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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