Open AccessDisplacement of Cortisol From Human Heart by Acute Administration of a Mineralocorticoid Receptor Antagonist
Author(s) -
Javaid Iqbal,
Ruth Andrew,
Nicholas L. Cruden,
Christopher J. Kenyon,
Katherine A. Hughes,
David E. Newby,
Patrick W. F. Hadoke,
Brian R. Walker
Publication year - 2013
Publication title -
the journal of clinical endocrinology and metabolism
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.206
H-Index - 353
eISSN - 1945-7197
pISSN - 0021-972X
DOI - 10.1210/jc.2013-2049
Subject(s) - mineralocorticoid receptor , mineralocorticoid , endocrinology , antagonist , medicine , displacement (psychology) , receptor antagonist , receptor , psychology , psychoanalysis
Mineralocorticoid receptor (MR) antagonists have beneficial effects in patients with heart failure and myocardial infarction, often attributed to blocking aldosterone action in the myocardium. However, binding of aldosterone to MR requires local activity of the enzyme 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), which inactivates cortisol to cortisone and thereby prevents receptor occupancy by cortisol. In vivo activity of 11β-HSD2 and potential occupancy of MR by cortisol in human heart have not been quantified.
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