Renal Aldosterone Receptors: Studies with [3H]Aldosterone and the Anti-Mineralocorticoid [3H]Spirolactone (SC-26304)

In vivo, a spirolactone (SC-26304) inhibited the effects of aldosterone on urinary K+:Na+ratios and the binding of [3H]aldosterone to renal cytoplasmic and nuclear receptors. Cytoplasmic binding of [3H]aldosterone and [3H]spirolactone (SC-26304) was similar in magnitude and involved the same set of...

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Bibliographic Details
Published in:Proceedings of the National Academy of Sciences - PNAS 1974-04, Vol.71 (4), p.1431-1435
Main Authors: Marver, Diana, Stewart, John, Funder, John W., Feldman, David, Edelman, Isidore S.
Format: Article
Language:English
Subjects:
Adrenalectomy
Aldosterone - metabolism
Animals
Binding Sites - drug effects
Binding, Competitive
Biological Sciences: Medical Sciences
Body weight
Cell Fractionation
Cell Nucleus - metabolism
Centrifugation
Centrifugation, Density Gradient
Chromatin
Cytoplasm
Cytoplasm - metabolism
Homogenization
In Vitro Techniques
Kidney - cytology
Kidney - drug effects
Kidney - metabolism
Kidney Function Tests
Kidneys
Lactones - pharmacology
Low concentrations
Mineralocorticoid Receptor Antagonists
Protein Binding
Rats
Receptors
Receptors, Cell Surface - drug effects
Salts
Spiro Compounds - pharmacology
Steroids
Tritium
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Summary:In vivo, a spirolactone (SC-26304) inhibited the effects of aldosterone on urinary K+:Na+ratios and the binding of [3H]aldosterone to renal cytoplasmic and nuclear receptors. Cytoplasmic binding of [3H]aldosterone and [3H]spirolactone (SC-26304) was similar in magnitude and involved the same set of sites. Under three sets of conditions--(i) in the intact rat, (ii) in kidney slices, and (iii) in reconstitution studies (mixing prelabeled cytoplasm with either purified renal nuclei or chromatin), [3H]spirolactone (SC-26304) did not yield specific nuclear complexes in contrast to the reproducible generation of these complexes with [3H]aldosterone. In glycerol density gradients, cytoplasmic [3H]aldosterone receptor complexes sedimented at 8.5 S and 4 S in low concentrations of salt and at 4.5 S in high concentrations of salt. Cytoplasmic [3H]spirolactone (SC-26304) receptor complexes sedimented at 3 S in low concentrations of salt and 4 S in high concentrations of salt. These results are discussed in terms of an allosteric model of the receptor system.
ISSN:0027-8424
1091-6490
DOI:10.1073/pnas.71.4.1431