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Ligand: aldosterone
INN: aldosterone
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Ligand: [3H]aldosterone
Synonyms: [3H]-aldosterone
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Ligand: lorundrostat
Comments: aldosterone synthase (CYP11B2) inhibitor. Reducing aldosterone biosynthesis is proposed as an alternative to mineralocorticoid receptor
Clinical use: Lorundrostat is a clinical candidate for the treatment of aldosterone-dependent treatment-resistant hypertension . Bioactivity comments: selective for aldosterone synthase (CYP11B2) compared to the highly homologous, cortisol-producing enzyme 11beta-hydroxylase (CYP11B1) . |
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Ligand: baxdrostat
Comments: aldosterone synthase (CYP11B2) inhibitor. It inhibits aldosterone biosynthesis but does not alter plasma cortisol, which
Clinical use: aldosterone levels in patients with primary aldosteronism/hyperaldosteronism. Pharmacokinetics and safety data from a phase 1 trial Bioactivity comments: aldosterone synthase (CYP11B2) compared to 11beta-hydroxylase (CYP11B1, which is responsible for cortisol biosynthesis) . Baxdrostat |
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Ligand: vicadrostat
Comments: aldosterone synthase (CYP11B2) inhibitor . Reducing aldosterone biosynthesis is proposed as an alternative to mineralocorticoid receptor
Bioactivity comments: aldosterone synthesis) compared to CYP11B1 (cortisol synthesis) . It does not significantly inhibit CYP17A1 or CYP19A1 |
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Ligand: osilodrostat
Comments: aldosterone synthase (CYP11B2), but is also reported to inhibit the closely related enzyme, 11-beta
Mechanism of action: aldosterone , a key hormone in the renin-angiotensin-aldosterone system (RAAS) which regulates blood pressure |
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Ligand: dexfadrostat
Comments: selectivity for aldosterone synthase (CYP11B2) compared to the highly homologous, cortisol-producing enzyme 11beta-hydroxylase (CYP11B1) .
Clinical use: treatment of primary aldosteronism (and its associated uncontrolled hypertension) and aldosterone-dependent treatment-resistant hypertension . |
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Ligand: eplerenone
Comments: Eplerenone is a potassium-sparing diuretic, which works by antagonising the effects of aldosterone.
Mechanism of action: aldosterone-system and increases blood pressure by several potential routes, including induction of sodium reabsorption |
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Ligand: spironolactone
Comments: potassium-sparing diuretic, which works by antagonising the effects of aldosterone at renal mineralocorticoid receptors.
Mechanism of action: aldosterone antagonist at the mineralocorticoid receptor in the cortical collecting duct of renal nephrons, an action |
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Ligand: fadrozole
Comments: aldosterone synthase) responsible for cortisol and aldosterone synthesis respectively . Fadrozole is a racemic mixture. Evidence
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