Premium
Bioassay of a new aldosterone antagonist and evaluation of a simple method of quantitative comparison
Author(s) -
McInnes Gordon T,
Shelton John R,
Asbury Michael J,
Harrison Ian R,
Clarke Joan M,
Ramsay Lawrence E,
Venning Geoffrey R
Publication year - 1981
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1981.151
Subject(s) - aldosterone , spironolactone , fludrocortisone , potency , bioassay , pharmacology , antagonist , confidence interval , chemistry , medicine , biology , receptor , biochemistry , hydrocortisone , in vitro , genetics
The renal antimineralocorticoid activity of single oral doses of a new aldosterone antagonist OH OPC(ME)‐K was compared to that of spironolactone in two studies in healthy men. OH OPC(ME)‐K reversed the urinary electrolyte response to fludrocortisone in the period up to 16 hr after treatment, but it was less potent than spironolactone on a weight basis. The best estimate of the relative potency of OH OPC(ME)‐K:spironolactone (derived from a simple protocol using equal single doses of the two drugs) was 0.60:1 (95% confidence limits 0.24:1 to 1.42:1), in good agreement with the estimate from a more complex three‐dose parallel‐line bioassay (0.61:1, 95% confidence limits 0.48:1 to 0.79:1). The results of simple single‐dose studies can be used, with certain assumptions, to provide a useful estimate of the relative potency of new aldosterone antagonists at an early stage of development. Clinical Pharmacology and Therapeutics (1981) 30, 218–225; doi: 10.1038/clpt.1981.151