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Review ArticleReview Article

Acute Alcohol Action and Desensitization of Ligand-Gated Ion Channels

Alex M. Dopico and David M. Lovinger
Pharmacological Reviews March 2009, 61 (1) 98-114; DOI: https://doi.org/10.1124/pr.108.000430
Alex M. Dopico
Department of Pharmacology, the University of Tennessee Health Science Center, Memphis, Tennessee (A.M.D.); and Laboratory for Integrative Neuroscience, National Institute on Alcohol Abuse and Alcoholism, Bethesda, Maryland (D.M.L.)
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David M. Lovinger
Department of Pharmacology, the University of Tennessee Health Science Center, Memphis, Tennessee (A.M.D.); and Laboratory for Integrative Neuroscience, National Institute on Alcohol Abuse and Alcoholism, Bethesda, Maryland (D.M.L.)
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Abstract

Ethanol exerts its biological actions through multiple receptors, including ion channels. Ion channels that are sensitive to pharmacologically relevant ethanol concentrations constitute a heterogeneous set, including structurally unrelated proteins solely sharing the property that their gating is regulated by a ligand(s). Receptor desensitization is almost universal among these channels, and its modulation by ethanol may be a crucial aspect of alcohol pharmacology and effects in the body. We review the evidence documenting interactions between ethanol and ionotropic receptor desensitization, and the contribution of this interaction to overall ethanol action on channel function. In some cases, such as type 3 serotonin, nicotinic acetylcholine, GABA-A, and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptors, ethanol actions on apparent desensitization play a significant role in acute drug action on receptor function. In a few cases, mutagenesis helped to identify different areas within a receptor protein that differentially sense n-alcohols, resulting in differential modulation of receptor desensitization. However, desensitization of a receptor is linked to a variety of biochemical processes that may alter protein conformation, such as the lipid microenvironment, post-translational channel modification, and channel subunit composition, the relative contribution of these processes to ethanol interactions with channel desensitization remains unclear. Understanding interactions between ethanol and ionotropic receptor desensitization may help to explain different ethanol actions 1) when ethanol is evaluated in vitro on cloned channel proteins, 2) under physiological or pathological conditions or in distinct cell domains with modified ligand concentration and/or receptor conformation. Finally, receptor desensitization is likely to participate in molecular and, possibly, behavioral tolerance to ethanol, which is thought to contribute to the risk of alcoholism.

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Pharmacological Reviews: 61 (1)
Pharmacological Reviews
Vol. 61, Issue 1
1 Mar 2009
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Review ArticleReview Article

Acute Alcohol Action and Desensitization of Ligand-Gated Ion Channels

Alex M. Dopico and David M. Lovinger
Pharmacological Reviews March 1, 2009, 61 (1) 98-114; DOI: https://doi.org/10.1124/pr.108.000430

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Review ArticleReview Article

Acute Alcohol Action and Desensitization of Ligand-Gated Ion Channels

Alex M. Dopico and David M. Lovinger
Pharmacological Reviews March 1, 2009, 61 (1) 98-114; DOI: https://doi.org/10.1124/pr.108.000430
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  • Article
    • Abstract
    • I. Introduction
    • II. Of Desensitization and Receptors
    • III. Ethanol and Desensitization of Receptor Channels of the Cys-Loop Family
    • IV. Ethanol and Desensitization of Glutamate-Activated Ligand-Gated Ion Channels
    • V. Ethanol and Desensitization of Extracellular ATP-Gated Ion Channels
    • VI. Ethanol and Desensitization of Potassium Channels That Are Gated by Intracellular Ligands
    • VII. Conclusions and Implications
    • Acknowledgments
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    • References
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