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PMID: 2413213 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Voltage dependence of Na channel blockage by amiloride: relaxation effects in admittance spectra.

The Journal of membrane biology ·Vol. 86 ·No. 3 ·1985-00-00 ·Pages 255-65

Warncke J, Lindemann B

Abstract

Amiloride, present in the mucosal solution, causes the appearance of a distinct additional dispersion in the admittance spectrum of the apical membrane of toad urinary bladder. The parameters of this dispersion (characteristic frequency, amplitude) change with amiloride concentration and with membrane voltage. They allow the calculation of the overall rate constants for Na channel blockage by the positively charged form of amiloride, and the voltage dependence of these rate constants. The on-rate of blockage increases and the off-rate decreases when the membrane surface to which cationic amiloride has access, is made more positive. This result is suggestive of a blocking model where the cationic amidino group of amiloride, depending on its charge, senses 10 to 13% of the membrane voltage while invading the channel entrance by a single-step process, and rests at an electrical distance corresponding to 24 to 30% of membrane voltage while occupying the blocking position.

MeSH Terms
Amiloride/pharmacology Animals Bufo marinus In Vitro Techniques Ion Channels/drug effects,physiology Kinetics Mathematics Membrane Potentials/drug effects Models, Biological Sodium/metabolism Software Urinary Bladder/drug effects,physiology
Chemicals
Ion Channels Amiloride Sodium
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Warncke J
Lindemann B
References (31)
31 references, click to expand
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Article Info
Journal
The Journal of membrane biology
Abbr.
J Membr Biol
ISSN
0022-2631
DOI
10.1007/BF01870605
Published
1985-00-00
Pages
255-65
Language
English
Region
United States
NLM ID
0211301
Subset
IM
External Links
PubMed source DOI: 10.1007/BF01870605 View journal details
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