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Competitive blocking of epithelial sodium channels by organic cations: The relationship between macroscopic and microscopic inhibition constants

The Journal of Membrane Biology, ISSN: 0022-2631, Vol: 76, Issue: 3, Page: 235-251
1983
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Fluctuation analysis of Na current passing the apical membrane in the skin of Rana ridibunda was used to study the kinetics of Na-channel blocking by several organic cations present in the outer solution together with 60 mm Na. The ratios of the apparent off-rate and on-rate constants (the microscopic inhibition constants) thus obtained for triamterene, triaminopyrimidine (TAP), 5,6-diCl-amiloride, 5H-amiloride and amiloride itself are found to be in the mean about sevenfold smaller than the corresponding inhibition constants obtained from macroscopic dose-response curves. The apparent discrepancy is explicable by competition of the organic blocker with the channel block by Na ions (the self-inhibition effect). The type of interaction between extrinsic blockage and self-inhibition may be purely competitive or mixed. However, in case of mixed inhibition the competitive component must dominate the noncompetitive component by at least seven to one. © 1983 Springer-Verlag.

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