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Mineralocorticoid receptor antagonist information


Mineralocorticoid receptor antagonist
Drug class
Spironolactone, the most widely used antimineralocorticoid.
Class identifiers
SynonymsAldosterone antagonistic; Mineralocorticoid antagonist
UseDiuretic; Chronic heart failure; Hypertension; Hyperaldosteronism; Conn's syndrome
Biological targetMineralocorticoid receptor
Chemical classSteroidal; Nonsteroidal
Legal status
In Wikidata

A mineralocorticoid receptor antagonist (MRA or MCRA)[1] or aldosterone antagonist, is a diuretic drug which antagonizes the action of aldosterone at mineralocorticoid receptors. This group of drugs is often used as adjunctive therapy, in combination with other drugs, for the management of chronic heart failure. Spironolactone, the first member of the class, is also used in the management of hyperaldosteronism (including Conn's syndrome) and female hirsutism (due to additional antiandrogen actions). Most antimineralocorticoids, including spironolactone, are steroidal spirolactones. Finerenone is a nonsteroidal antimineralocorticoid.

  1. ^ The Krause/King-Lewis acronym, developed at Naval Medical Center San Diego Archived 2018-07-13 at the Wayback Machine, of MCRA was developed during February 2017 to distinguish between MRA for a specific MRI which are both widely recognized medical acronyms as compared to the use of MRA for mineralocorticoid receptor antagonist type medications which is only used as a medical acronym in the cardiology and nephrology word.

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Mineralocorticoid receptor antagonist

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A mineralocorticoid receptor antagonist (MRA or MCRA) or aldosterone antagonist, is a diuretic drug which antagonizes the action of aldosterone at mineralocorticoid...

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Mineralocorticoid receptor

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The mineralocorticoid receptor (or MR, MLR, MCR), also known as the aldosterone receptor or nuclear receptor subfamily 3, group C, member 2, (NR3C2) is...

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Finerenone

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associated with type 2 diabetes. Finerenone is a non-steroidal mineralocorticoid receptor antagonist (MRA). It is taken orally (swallowed by mouth). Common side...

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Mineralocorticoid

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potassium levels. The effects of mineralocorticoids are mediated by slow genomic mechanisms through nuclear receptors as well as by fast nongenomic mechanisms...

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Heart failure

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angiotensin receptor blockers, or angiotensin receptor-neprilysin inhibitors, along with beta blockers, mineralocorticoid receptor antagonists and SGLT2...

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Bärfacker L (July 2017). "30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development". J...

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treatment of hypertension. Aldosterone receptor antagonists, also known as mineralocorticoid receptor antagonist (MRA) can lower blood pressure by blocking...

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Heart failure with preserved ejection fraction

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ACE inhibitors, calcium channel blockers, beta blockers, and angiotensin receptor blockers is employed, but does not have a proven benefit in HFpEF patients...

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Ocedurenone

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formerly known as KBP-5074, is a nonsteroidal, selective mineralocorticoid receptor antagonist that is being developed to treat hypertension in patients...

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Eplerenone

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selective aldosterone receptor antagonist (SARA). Eplerenone is more selective than spironolactone at the mineralocorticoid receptor relative to binding...

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Membrane mineralocorticoid receptor

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Membrane mineralocorticoid receptors (mMRs) or membrane aldosterone receptors are a group of receptors which bind and are activated by mineralocorticoids such...

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acuity compared to control patients. Spironolactone is a mineralocorticoid receptor antagonist that may help reduce the fluid associated with CSR. In a...

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hormone receptors, and is known to possess the following activities: Mineralocorticoid receptor antagonist (Ki = 39 nM) Progesterone receptor partial...

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Spironolactone

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Bärfacker L (July 2017). "30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development". The...

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Esaxerenone

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silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over...

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Apparent mineralocorticoid excess syndrome

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concentrations can cross-react and activate the mineralocorticoid receptor due to the non-selectivity of the receptor, leading to aldosterone-like effects in...

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ARA

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II receptor antagonist, more often called angiotensin receptor blocker (ARB) Aldosterone receptor antagonist (mineralocorticoid receptor antagonist, that...

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MRA

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MRA may refer to: Magnetic resonance angiography Mineralocorticoid receptor antagonist Monoamine releasing agent Multiresolution analysis Madison-Ridgeland...

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Nuclear receptor

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binding site in the nuclear receptor. These ligands are referred to as antagonists. An example of antagonistic nuclear receptor drug is mifepristone which...

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Apararenone

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Apararenone acts as a highly selective antagonist of the mineralocorticoid receptor (Ki < 50 nM), the receptor for aldosterone. As of 2017, it is in phase...

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Aldosterone

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potassium (K+) levels. It does so primarily by acting on the mineralocorticoid receptors in the distal tubules and collecting ducts of the nephron. It...

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Daiichi Sankyo Initiates Phase 3 study of CS-3150, a Novel Mineralocorticoid Receptor Antagonist for Treatment of Essential Hypertension". Daiichi Sankyo...

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trials: †Phase III §Never to phase III See also Glucocorticoid receptor modulators Mineralocorticoids and antimineralocorticoids List of corticosteroids...

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Receptor modulator

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efficacy. Categories of these modulators include receptor agonists and receptor antagonists, as well as receptor partial agonists, inverse agonists, orthosteric...

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Balcinrenone

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selective mineralocorticoid receptor modulator developed by AstraZeneca for heart failure. Compared to mineralocorticoid receptor antagonists, it is hoped...

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Pharmacodynamics of spironolactone

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a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor". J. Med. Chem. 50 (26): 6443–5. doi:10.1021/jm701186z...

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Feminizing hormone therapy

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