-transparent.png){kind=logo}
The role of the soluble pool (cytoplasmic or cytosolic) of [3H]-aldosterone binding sites in the toad bladder was assessed by the use of two spirolactones, prorenone and spironolactone as a reference drug. Prorenone fulfills all the criteria for a specific competitive antagonist of aldosterone for its effect on Na+ transport. Compared with spironolactone (Ki approximately equal to 1 microM), prorenone was about eightfold less potent (Ki approximately equal to 8 microM). Competition for [3H]aldosterone binding sites by spironolactone and prorenone revealed an order of potency (spironolactone greater than prorenone) that corresponded to their antagonist activities in the Na+ transport assay. There was a linear correlation between the effects of the two spirolactones on the aldosterone-stimulated Na+ transport and their ability to displace [3H]aldosterone from its binding sites in the soluble pool. Finally [3H]prorenone binding sites were detected in the soluble pool but an insignificant number of antagonist-receptor complexes were found associated with the nuclear pool. Our study indicates that the aldosterone binding sites of the soluble pool are indeed mineralocorticoid receptors, which are probably the first intracellular mediators leading to an increased Na+ reabsorption.
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
July 1976,
The American journal of physiology,
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
July 1976,
Journal of medicinal chemistry,
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
October 1977,
Journal of medicinal chemistry,
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
May 2001,
Molecular pharmacology,
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
December 1968,
The Biochemical journal,
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
January 1967,
Biochimica et biophysica acta,
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
September 1981,
Journal of medicinal chemistry,
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
November 1969,
Biochimica et biophysica acta,
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
January 1984,
The American journal of physiology,
B C Rossier, and
M Claire, and
M E Rafestin-Oblin, and
K Geering, and
H P Gäggeler, and
P Corvol
April 1966,
The Journal of clinical investigation,
