Binding of loop diuretics to their renal receptors: use as a screening model for potential diuretic activity

Loop diuretics of the benzoic acid and aryloxyacetic acid families inhibit Na+K+Cl- cotransport. The ranking order of potencies measured in the thick ascending limb of Henle's loop and the ranking order of affinities for [3H]piretanide receptors on renal plasma membranes are the same. Potencies...

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Bibliographic Details
Published inFundamental & clinical pharmacology Vol. 2; no. 3; p. 145
Main Authors Giesen-Crouse, E, Fandeleur, P, Welsch, C, Englert, H, Lang, H J, Schmidt, M, Imbs, J L
Format Journal Article
LanguageEnglish
Published England 01.01.1988
Subjects
Animals
Benzoates - therapeutic use
Diuretics - metabolism
Diuretics - therapeutic use
Dogs
Drug Evaluation, Preclinical - methods
In Vitro Techniques
Kidney - analysis
Loop of Henle - drug effects
Male
Receptors, Drug - metabolism
Sulfonamides - metabolism
Tritium
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Summary:Loop diuretics of the benzoic acid and aryloxyacetic acid families inhibit Na+K+Cl- cotransport. The ranking order of potencies measured in the thick ascending limb of Henle's loop and the ranking order of affinities for [3H]piretanide receptors on renal plasma membranes are the same. Potencies and affinities correlate well (correlation coefficient r = 0.959 for the medulla and r = 0.951 for the cortex). Therefore, measurement of [3H]piretanide binding is proposed to facilitate screening for loop diuretic action.
ISSN:0767-3981
DOI:10.1111/j.1472-8206.1988.tb00628.x