Abstract
Ion channels gated by neurotransmitters are present across metazoans, in which they are essential for brain function, sensation and locomotion; closely related homologs are also found in bacteria. Structures of eukaryotic pentameric cysteine-loop (Cys-loop) receptors and tetrameric ionotropic glutamate receptors in multiple functional states have recently become available. Here, I describe how these studies relate to established ideas regarding receptor activation and how they have enabled decades' worth of functional work to be pieced together, thus allowing previously puzzling aspects of receptor activity to be understood.
Publication types
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Review
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Bacteria / chemistry
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Bacteria / metabolism
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Benzothiadiazines / pharmacology
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Cognition / drug effects
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Cognition / physiology
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Cysteine Loop Ligand-Gated Ion Channel Receptors / chemistry*
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Cysteine Loop Ligand-Gated Ion Channel Receptors / genetics
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Cysteine Loop Ligand-Gated Ion Channel Receptors / metabolism
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Gene Expression
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Humans
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Ion Channel Gating / drug effects
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Ion Channels / chemistry*
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Ion Channels / genetics
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Ion Channels / metabolism
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Ivermectin / pharmacology
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Locomotion / drug effects
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Locomotion / physiology
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Models, Molecular
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Neurotransmitter Agents / metabolism*
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Perception / drug effects
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Perception / physiology
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Piperidines / pharmacology
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Receptors, Glutamate / chemistry*
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Receptors, Glutamate / genetics
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Receptors, Glutamate / metabolism
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Synapses / drug effects
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Synapses / metabolism*
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Synaptic Transmission / drug effects
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Synaptic Transmission / physiology*
Substances
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Benzothiadiazines
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Cysteine Loop Ligand-Gated Ion Channel Receptors
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Ion Channels
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Neurotransmitter Agents
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Piperidines
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Receptors, Glutamate
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Ivermectin
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cyclothiazide
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ifenprodil