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Interplay between Gating and Block of Ligand-Gated Ion Channels

Phillips, Matthew B. and Nigam, Aparna and Johnson, Jon W. (2020) Interplay between Gating and Block of Ligand-Gated Ion Channels. Brain Sciences, 10 (12). p. 928. ISSN 2076-3425

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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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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
Phillips, Matthew
Nigam, Aparnaapn20@pitt.eduapn20
Johnson, Jon W.jjohnson@pitt.edujjohnson
Centers: Other Centers, Institutes, Offices, or Units > Center for Neuroscience
Date: 1 December 2020
Date Type: Publication
Journal or Publication Title: Brain Sciences
Volume: 10
Number: 12
Publisher: MDPI AG
Page Range: p. 928
DOI or Unique Handle: 10.3390/brainsci10120928
Schools and Programs: Dietrich School of Arts and Sciences > Neuroscience
Refereed: Yes
Uncontrolled Keywords: ligand-gated ion channel, channel block, channel gating, nicotinic acetylcholine receptor, ionotropic glutamate receptor, AMPA receptor
ISSN: 2076-3425
Official URL:
Funders: The National Institute of General Medical Sciences, The National Institute of Neurological Disorders and Stroke
Article Type: Review
Date Deposited: 02 Jun 2021 19:21
Last Modified: 02 Jun 2021 19:21


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