Bioassay of a new aldosterone antagonist and evaluation of a simple method of quantitative comparison

Autor: Geoffrey R Venning, Joan M Clarke, JR Shelton, Gordon T McInnes, Ian R Harrison, LE Ramsay, Michael J Asbury
Rok vydání: 1981
Předmět:
Zdroj: Clinical pharmacology and therapeutics. 30(2)
ISSN: 0009-9236
Popis: 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
Databáze: OpenAIRE