Interplay between Gating and Block of Ligand-Gated Ion Channels
1
Department of Neuroscience, University of Pittsburgh, Pittsburgh, PA 15260, USA
2
Center for Neuroscience, University of Pittsburgh, Pittsburgh, PA 15260, USA
*
Author to whom correspondence should be addressed.
Brain Sci. 2020, 10(12), 928; https://doi.org/10.3390/brainsci10120928
Received: 27 October 2020 / Revised: 21 November 2020 / Accepted: 26 November 2020 / Published: 1 December 2020
(This article belongs to the Special Issue A Decade of Brain Sciences)
Drugs that inhibit ion channel function by binding in the channel and preventing current flow, known as channel blockers, can be used as powerful tools for analysis of channel properties. Channel blockers are used to probe both the sophisticated structure and basic biophysical properties of ion channels. Gating, the mechanism that controls the opening and closing of ion channels, can be profoundly influenced by channel blocking drugs. Channel block and gating are reciprocally connected; gating controls access of channel blockers to their binding sites, and channel-blocking drugs can have profound and diverse effects on the rates of gating transitions and on the stability of channel open and closed states. This review synthesizes knowledge of the inherent intertwining of block and gating of excitatory ligand-gated ion channels, with a focus on the utility of channel blockers as analytic probes of ionotropic glutamate receptor channel function.
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Keywords:
ligand-gated ion channel; channel block; channel gating; nicotinic acetylcholine receptor; ionotropic glutamate receptor; AMPA receptor; kainate receptor; NMDA receptor
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MDPI and ACS Style
Phillips, M.B.; Nigam, A.; Johnson, J.W. Interplay between Gating and Block of Ligand-Gated Ion Channels. Brain Sci. 2020, 10, 928. https://doi.org/10.3390/brainsci10120928
AMA Style
Phillips MB, Nigam A, Johnson JW. Interplay between Gating and Block of Ligand-Gated Ion Channels. Brain Sciences. 2020; 10(12):928. https://doi.org/10.3390/brainsci10120928
Chicago/Turabian StylePhillips, Matthew B.; Nigam, Aparna; Johnson, Jon W. 2020. "Interplay between Gating and Block of Ligand-Gated Ion Channels" Brain Sci. 10, no. 12: 928. https://doi.org/10.3390/brainsci10120928
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