General anaesthetic actions on ligand-gated ion channels
Open accessAbstract
The molecular mechanisms of general anaesthetics have remained largely obscure since their introduction into clinical practice just over 150 years ago. This review describes the actions of general anaesthetics on mammalian neurotransmitter-gated ion channels. As a result of research during the last several decades, ligand-gated ion channels have emerged as promising molecular targets for the central nervous system effects of general anaesthetics. The last 10 years have witnessed an explosion of studies of anaesthetic modulation of recombinant ligand-gated ion channels, including recent studies which utilize chimeric and mutated receptors to identify regions of ligand-gated ion channels important for the actions of general anaesthetics. Exciting future directions include structural biology and gene-targeting approaches to further the understanding of general anaesthetic molecular mechanisms.
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GABAA receptors contribute to sedation, hypnosis, hypothermia, and immobility, based on knock-in mice with point mutations that abolish anesthetic binding sites and reduce behavioral effects.
“Convincing evidence for a contribution of GABAA receptors to important anesthetic actions such as sedation, hypnosis, hypothermia, and immobility have come from experiments on knock-in mice, in which point mutations that abolish anesthetic binding sites also curtail the behavioral effects of several anesthetics [38, 39].”
From The Biology of General Anesthesia from Paramecium to Primate (2019) · cites this paper as [39]
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Self-citationDoes the Immobilizing Effect of Thiopental in Brain Exceed That of Halothane?
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- Authors
- Krasowski, M. D., & Harrison, N. L.
- Affiliations
- University of Chicago (US)
- Venue
- Cellular and Molecular Life Sciences (CMLS)
- Published
- 1999-08-01
- Volume
- 55
- Issue
- 10
- Pages
- 1278-1303
- ISSN
- 1420-682X (ISSN-L)
- 1420-9071
- PMC
- PMC2854026
- OpenAlex
- W2088909919
- Cited by
- 384
- References
- 346
- Citations by year
- 2026: 2 · 2025: 8 · 2024: 6 · 2023: 5 · 2022: 5 · 2021: 9 · 2020: 12 · 2019: 8 · 2018: 7 · 2017: 13 · 2016: 10 · 2015: 12 · 2014: 14 · 2013: 12 · 2012: 14
- FWCI
- 5.40
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Cellular and Molecular Life Sciences (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (7r01gm056850-03, 5k04gm000623-04)
- National Institute of Mental Health (F30MH011504)
- National Institute of General Medical Sciences (GM-45129, R01GM045129, GM56850, GM00623)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Health Sciences › Medicine › Anesthesiology and Pain Medicine › Anesthesia and Sedative Agents
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Keywords
- general anesthetics, ligand-gated ion channels, anesthetic mechanisms, chimeric receptors, receptor mutations
- MeSH terms
- Animals, Cell Membrane, Humans, Ion Channels, Ligands, Mammals, Protein Conformation, Receptors, Cell Surface, Ion Channel Gating, Anesthetics, General
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