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. 1982 Mar;13(3):331–339. doi: 10.1111/j.1365-2125.1982.tb01383.x

Relative potency and structure activity relationships of aldosterone antagonists in healthy man: correlation with animal experience.

G T McInnes, J R Shelton, L E Ramsay, I R Harrison, M J Asbury, J M Clarke, R M Perkins, G R Venning
PMCID: PMC1402118  PMID: 6460516

Abstract

1 The renal antimineralocorticoid potency of single doses of thirteen compounds with properties in animals compatible with competitive aldosterone antagonism was compared to that of spironolactone in healthy men. 2 Twelve compounds showed significant activity when compared to placebo but only one, prorenoate potassium, was significantly more potent than spironolactone on a weight basis. 3 The results allowed ranking of the compounds in order of potency relative to spironolactone and general observations on structure activity relationships in man. 4 Animal bioassays and in vitro aldosterone binding studies are unreliable predictors of the human activity of competitive mineralocorticoid antagonists.

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Selected References

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