Interaction of Tetraethylammonium Ion Derivatives with the Potassium Channels of Giant Axons
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A number of compounds related to TEA+ (tetraethylammoniumion) were injected into squid axons and their effects on gK (the potassium conductance) were determined. In most of these ions a quaternary nitrogen is surrounded by three ethyl groups and a fourth group that is very hydrophobic. Several of the ions cause inactivation of gK, a type of ionic gating that is not normally seen in squid axon; i.e., after depolarization gK increases and then spontaneously decreases to a small fraction of its peak value even though the depolarization is maintained. Observations on the mechanism of this gating show that (a) QA (quaternary ammonium) ions only enter K+ channels that have open activation gates (the normal permeability gates). (b) The activation gates of QA-occluded channels do not close readily. (c) Hyperpolarization helps to clear QA ions from the channels. (d) Raising the external K+ concentration also helps to clear QA ions from the channels. Observations (c) and (d) strongly suggest that K+ ions traverse the membrane by way of pores, and they cannot be explained by the usual type of carrier model. The data suggest that a K+ pore has two distinct parts: a wide inner mouth that can accept a hydrated K+ ion or a TEA+-like ion, and a narrower portion that can accept a dehydrated or partially dehydrated K+ ion, but not TEA+.
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Quaternary amines with substantial hydrophobic substituents display detectable membrane permeability.
“Quaternary amines with substantial hydrophobic substituents also display detectable membrane permeability; this is revealed in the literature on blockers of voltage-gated ion channels.”
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- Authors
- Armstrong, C. M.
- Affiliations
- University of Rochester Medicine (US)
- Corresponding author
- Armstrong, Clay M.
- Venue
- The Journal of General Physiology
- Publisher
- Rockefeller University Press
- Published
- 1971-10-01
- Volume
- 58
- Issue
- 4
- Pages
- 413-437
- ISSN
- 0022-1295 (ISSN-L)
- 1540-7748
- PMC
- PMC2226036
- OpenAlex
- W2006090981
- Cited by
- 929
- References
- 23
- Citations by year
- 2026: 4 · 2025: 11 · 2024: 6 · 2023: 7 · 2022: 8 · 2021: 10 · 2020: 9 · 2019: 9 · 2018: 11 · 2017: 13 · 2016: 14 · 2015: 15 · 2014: 14 · 2013: 14 · 2012: 33
- FWCI
- 4.49
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- The Journal of General Physiology (publishedVersion)
- PubMed Central (publishedVersion, cc-by-nc-sa)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion Transport and Channel Regulation
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Keywords
- tetraethylammonium, quaternary ammonium ions, potassium channels, potassium conductance, channel inactivation, ion gating, activation gate, pore model, potassium ion permeation, hyperpolarization, external potassium concentration, squid giant axon, ion selectivity
- MeSH terms
- Animals, Axons, Cell Membrane Permeability, Ion Exchange, Ions, Membrane Potentials, Models, Biological, Mollusca, Potassium, Tetraethylammonium Compounds, In Vitro Techniques
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