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BINDING OF LOOP DIURETICS TO THEIR RENAL RECEPTORS: USE AS A SCREENING MODEL FOR POTENTIAL DIURETIC ACTIVITY
Author(s) -
GIESENCROUSE E.,
FANDELEUR P.,
WELSCH C.,
ENGLERT H.,
LANG H.J.,
SCHMIDT M.,
IMBS J.L.
Publication year - 1988
Publication title -
fundamental and clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.655
H-Index - 73
eISSN - 1472-8206
pISSN - 0767-3981
DOI - 10.1111/j.1472-8206.1988.tb00628.x
Subject(s) - diuretic , loop of henle , chemistry , affinities , receptor , endocrinology , bumetanide , cotransporter , pharmacology , medicine , biochemistry , sodium , biology , renal function , nephron , organic chemistry
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 [ 3 H]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 [ 1 H]piretanide binding is proposed to facilitate screening for loop diuretic action.