Abstract
Local anesthetics inhibit the ion channel activity of nicotinic acetylcholine receptors in a noncompetitive fashion. This inhibitory action is ascribed to two possible inhibitory mechanisms: an open-channel-blocking mechanism and/or an allosteric process where the drug binds either to the closed channel or to other nonluminal sites, respectively.
Publication types
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Research Support, U.S. Gov't, P.H.S.
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Review
MeSH terms
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Allosteric Regulation / drug effects
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Anesthetics, Local / chemistry*
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Anesthetics, Local / pharmacology
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Animals
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Humans
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Ion Channels / antagonists & inhibitors*
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Membrane Potentials / drug effects
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Nicotinic Antagonists / chemistry
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Nicotinic Antagonists / pharmacology
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Receptors, Nicotinic / chemistry
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Receptors, Nicotinic / drug effects*
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Receptors, Nicotinic / physiology
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Structure-Activity Relationship
Substances
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Anesthetics, Local
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Ion Channels
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Nicotinic Antagonists
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Receptors, Nicotinic