Why the study?
Do new aldosterone antagonists improve renal antimineralocorticoid potency compared to spironolactone in healthy men?
Do new aldosterone antagonists improve renal antimineralocorticoid potency compared to spironolactone in healthy men?
Animal bioassays and in vitro binding studies are unreliable predictors of human antimineralocorticoid potency, highlighting the need for human testing of aldosterone antagonists.
Supports human trials of prorenoate potassium for superior potency; challenges reliance on animal bioassays for predicting aldosterone antagonist effects in humans.
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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McInnes et al. (1982) studied this question.
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