Abstract
After incorporation of purified sheep cardiac Ca(2+)-release channels into planar phospholipid bilayers, we have investigated the blocking effects of a series of monovalent (CH3-(CH2)n-1-N+(CH3)3) and divalent ((CH3)3N(+)-(CH2)n-N+(CH3)3) trimethylammonium derivatives under voltage clamp conditions. All the compounds tested produce voltage-dependent block from the cytoplasmic face of the channel. With divalent (Qn) derivatives the effective valence of block decreases with increasing chain length, reaching a plateau with a chain length of n > or = 7. No decline in effective valence is observed with the monovalent (Un) derivatives. A plausible interpretation of this phenomena suggests that for the 90% of the voltage drop measured, the increase in length following the addition of a CH2 in the chain spans 12.7% of the electrical field. Extrapolating this distance to include the remaining 10% suggests that the applied holding potential falls over a total distance of 10.4 A. In addition, at high positive holding potentials there is evidence for permeation of the trimethylammonium ions and a valency specific relief of block.
MeSH Terms
Animals
Biophysical Phenomena
Biophysics
Calcium Channel Blockers/chemistry,pharmacology
Calcium Channels/chemistry,isolation & purification
Electrochemistry
In Vitro Techniques
Ion Channels/chemistry
Lipid Bilayers
Membrane Potentials
Molecular Structure
Muscle Proteins/chemistry,isolation & purification
Myocardium/chemistry
Quaternary Ammonium Compounds/chemistry,pharmacology
Ryanodine Receptor Calcium Release Channel
Sarcoplasmic Reticulum/chemistry
Sheep
Chemicals
Calcium Channel Blockers
Calcium Channels
Ion Channels
Lipid Bilayers
Muscle Proteins
Quaternary Ammonium Compounds
Ryanodine Receptor Calcium Release Channel
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Tinker A
Department of Cardiac Medicine, National Heart and Lung Institute, University of London, United Kingdom.
Williams A J
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