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Mineralocorticoid Receptor Blockers: Novel Selective Nonsteroidal Mineralocorticoid Receptor Antagonists

Current Hypertension Reports, 2020
Recently, nonsteroidal mineralocorticoid receptor (MR) antagonists (MRAs), which have been proposed to be called MR blockers (MRBs), have become available for clinical use, but their clinical role is unknown. We reviewed the clinical roles of MRAs and MRBs based on previous knowledge and as demonstrated in representative clinical trials.Steroidal MRAs,
Daisuke, Sueta   +2 more
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Mineralocorticoid Receptor Antagonists

2019
Two mineralocorticoid receptor antagonists, spironolactone and eplerenone, are currently approved by the FDA. Several non-steroid based ligands are in clinical trials for indications including heart failure, hypertension and diabetic kidney disease, and even more structurally distinct chemical series are reported in the literature with preclinical data
Anneli, Nordqvist, Kenneth L, Granberg
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Adipocyte Mineralocorticoid Receptor

2019
Mineralocorticoid receptor (MR) has been recently identified in adipose tissue, where its excessive activation contributes to several metabolic derangements often observed in obesity and metabolic syndrome. Recent findings support the existence of a bidirectional cross-talk between adipose tissue and adrenal glands, contributing to obesity-related ...
Infante M.   +4 more
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Pseudohypoaldosteronism and mineralocorticoid receptor abnormalities

The Journal of Steroid Biochemistry and Molecular Biology, 1991
Pseudohypoaldosteronism is a rare inherited disease characterized by renal salt loss, hyperkalemia and metabolic acidosis despite highly elevated aldosterone values. We previously reported absent or reduced numbers of mineralocorticoid receptors in mononuclear leukocytes and defective effector mechanism as shown by no response in vitro to the ...
ARMANINI, DECIO   +8 more
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Mineralocorticoid receptor and cardiac arrhythmia

Clinical and Experimental Pharmacology and Physiology, 2013
Summary  Mineralocorticoid receptor (MR) activation has been shown to play a deleterious role in the development of heart disease in studies using specific MR antagonists (spironolactone, eplerenone) in both experimental models and patients. Pharmacological MR blockade attenuates the transition to heart failure (HF) in models of systolic left ...
Basile, Gravez   +2 more
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Interdomain interactions in the mineralocorticoid receptor

Molecular and Cellular Endocrinology, 2003
The potential for interaction between the N-terminal domain and the C-terminal region (hinge and ligand-binding domain) of the mineralocorticoid receptor (MR) was examined using the mammalian-2-hybrid assay. The MR C-terminal region was fused to the GAL4 DNA-binding domain (GAL4-MRC).
Fraser M, Rogerson, Peter J, Fuller
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Glucocorticoid and mineralocorticoid receptors for aldosterone

Journal of Steroid Biochemistry, 1972
Abstract Specific binding of aldosterone and dexamethasone by rat kidney and hepatoma tissue culture (HTC) cell cytosol has been studied. In cytosol of HTC cells, aldosterone and dexamethasone bind to a single class of sites with affinities that correspond with their potencies as inducers of tyrosine aminotransferase.
G, Rousseau   +4 more
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Reconsidering the Roles of the Mineralocorticoid Receptor

Hypertension, 2009
Translational research is usually taken to mean the application of laboratory discovery to clinical practice. Like languages or enzymes, however, translation is a 2-way street, and in the field of aldosterone and mineralocorticoid receptors (MR), there are a number of examples where clinical studies have prompted reconsideration of the basic biology ...
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[Mineralocorticoid receptor].

Nihon rinsho. Japanese journal of clinical medicine, 2009
Recent clinical trials have indicated the utility of mineralocorticoid receptor (MR) antagonists in patients with cardiovascular and renal diseases. Experiments studies have shown that chronic treatment with aldosterone resulted in severe cardiac and renal injuries, which were ameliorated by MR antagonists.
Akira, Nishiyama   +2 more
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Mineralocorticoid Receptors: Distribution and Activation

Heart Failure Reviews, 2005
Mineralocorticoid receptors (MR) bind both mineralocorticoids and glucocorticoids with high affinity (deoxycorticosterone = corticosterone >/= aldosterone = cortisol), and are found in both Na(+) transporting epithelia (e.g. kidney, colon) and nonepithelial tissues (e.g. heart, brain).
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