Quaternary Ammonium Compounds as Water Channel Blockers
نویسندگان
چکیده
From the Department of Physiology, Nijmegen Center for Molecular Life Sciences, Radboud University Nijmegen Medical Center, 6500 HB Nijmegen, Nijmegen, The Netherlands, the Max-Planck Institute for Biophysical Chemistry, Theoretical and Computational Biophysics Department, Am Fassberg, D-37077, Göttingen, Germany, and the Department of Chemistry, University of Edinburgh, Kings Buildings, West Mains Road, EH9 3JJ Scotland, United Kingdom
منابع مشابه
Trapping of Organic Blockers by Closing of Voltage-dependent K+ Channels
Small organic molecules, like quaternary ammonium compounds, have long been used to probe both the permeation and gating of voltage-dependent K+ channels. For most K+ channels, intracellularly applied quaternary ammonium (QA) compounds such as tetraethylammonium (TEA) and decyltriethylammonium (C10) behave primarily as open channel blockers: they can enter the channel only when it is open, and ...
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Polymeric maleimido-quaternary ammonium (QA) compounds have been shown to function as molecular tape measures when covalently tethered to external cysteine residues of a Shaker K(+) channel (Blaustein R.O., P.A. Cole, C. Williams, and C. Miller. 2000. Nat. Struct. Biol. 7:309-311). For sufficiently long compounds, the cysteine-maleimide tethering reaction creates a high concentration, at the ch...
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Use-dependent blockers and exit rate of the last ion from the multi-ion pore of a K+ channel.
Quaternary ammonium blockers inhibit many voltage-activated potassium (K+) channels from the intracellular side. When applied to Drosophila Shaker potassium channels expressed in mammalian cells, these rapidly reversible blockers produced use-dependent inhibition through an unusual mechanism--they promoted an intrinsic conformational change known as C-type inactivation, from which recovery is s...
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A series of n-alkyl-bis-alpha,omega-trimethylammonium (bisQn) compounds was synthesized, and their ability to block K+ currents through a K+ channel from sarcoplasmic reticulum was studied. K+ channels were inserted into planar phospholipid membranes, and single-channel K+ currents were measured in the presence of the blocking cations. These bisQn compounds block K+ currents only from the side ...
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