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Published on: January 27, 2013
Binding of loop diuretics to their renal receptors: use as a screening model for potential diuretic activity
E Giesen-Crouse1, P Fandeleur, C Welsch
1Institut de Pharmacologie (UA 589 CNRS), Faculté de Médecine, Strasbourg, France.
Abstract:
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.
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