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 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.
Giesen-Crouse
E
E
Institut de Pharmacologie (UA 589 CNRS), Faculté de Médecine, Strasbourg, France.
Fandeleur
P
P
Welsch
C
C
Englert
H
H
Lang
H J
HJ
Schmidt
M
M
Imbs
J L
JL
D000818:Animals; D001565:Benzoates / Q000627:therapeutic use; D004232:Diuretics / Q000378:metabolism / Q000627:therapeutic use*; D004285:Dogs; D004353:Drug Evaluation, Preclinical / Q000379:methods; D066298:In Vitro Techniques; D007668:Kidney / Q000032:analysis*; D008138:Loop of Henle / Q000187:drug effects; D008297:Male; D011955:Receptors, Drug / Q000378:metabolism*; D013449:Sulfonamides / Q000378:metabolism; D014316:Tritium
D001565:Benzoates; D004232:Diuretics; D011955:Receptors, Drug; D013449:Sulfonamides; D014316:Tritium; C015451:piretanide