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- W2038107284 abstract "Abstract Anaesthetic agents range from simple inert gases to complex synthetic compounds. It is difficult to envisage a unifying mechanism by which all of these agents induce anaesthesia. This review is focused on ligand-gated ion channels. We introduce the molecular classification (plus the concept of superfamilies and receptor isomerism) and nomenclature of the pore-forming proteins, then overview the large body of recent data suggesting they may be selective anaesthetic targets. A wide variety of anaesthetics (volatiles, propofol, etomidate, neurosteroids and barbiturates) have been shown to interact with GABA A receptors. Point mutations in membrane spanning subunits comprising circa 450 amino acids can ablate the sensitivity of recombinant channels suggesting that the site of action is not in bulk membrane or interfacial lipids. Such drugs act stereoselectively to enhance the amplitude and or duration of inhibitory synaptic currents. In contrast, ketamine, nitrous oxide and xenon produce their anaesthetic effects (and untoward side effects) by depressing activity in the glutamatergic NMDA receptor. A minority of energetic researchers suggest that NMDA receptor activity is crucial for arousal (plays a more pivotal role in anaesthesia) and others suggest that voltage-gated channels are equally important in depressant drug action. Molecular biology and electrophysiology have been crucial for our understanding of channel function, but no concensus mechanism for anaesthetic action has yet emerged." @default.
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- W2038107284 date "2002-12-01" @default.
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- W2038107284 title "Ligand Gated Ion channels: crucial targets for anaesthetics?" @default.
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- W2038107284 doi "https://doi.org/10.1054/cacc.2003.0425" @default.
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