What is a glucocorticoid receptor antagonist?
In Wikidata. An antiglucocorticoid is a drug which reduces glucocorticoid activity in the body. They include direct glucocorticoid receptor antagonists such as mifepristone and synthesis inhibitors such as metyrapone, ketoconazole, and aminoglutethimide. They are used to treat Cushing’s syndrome.
Is mifepristone a glucocorticoid receptor antagonist?
Mifepristone, a glucocorticoid receptor antagonist, produces clinical and metabolic benefits in patients with Cushing’s syndrome. J Clin Endocrinol Metab. 2012 Jun;97(6):2039-49.
Is prednisone an agonist or antagonist?
Prednisolone, dexamethasone, and cortisol are all glucocorticoid receptor agonists, progesterone is a glucocorticoid receptor antagonist, and aldosterone has a hemiketyl group on C11, which renders it resistant to the action of 11β-hydroxysteroid dehydrogenase 2, enabling aldosterone to evade the action of this enzyme …
Which agonist does the glucocorticoid receptor bind to?
Agonists and antagonists Dexamethasone and other corticosteroids are agonists, while mifepristone and ketoconazole are antagonists of the GR.
Is cortisol an agonist or antagonist?
Prednisolone, dexamethasone, and cortisol are all glucocorticoid receptor agonists, progesterone is a glucocorticoid receptor antagonist, and aldosterone has a hemiketyl group on C11, which renders it resistant to the action of 11β- hydroxysteroid dehydrogenase 2, enabling aldosterone to evade the action of this enzyme …
Are corticosteroids agonists or antagonists?
Is dexamethasone an agonist?
Pharmacology. As a glucocorticoid, dexamethasone is an agonist of the glucocorticoid receptor (GR).
Is the glucocorticoid receptor a nuclear receptor?
The glucocorticoid receptor (GR) is an evolutionally conserved nuclear receptor superfamily protein that mediates the diverse actions of glucocorticoids as a ligand-dependent transcription factor.
Is adrenaline a glucocorticoid?
The hormones secreted from the cortex are steroids, generally classified as glucocorticoids (e.g., cortisol) and mineralocorticoids (e.g., aldosterone, which causes sodium retention and potassium excretion by the kidney). Those substances emanating from the medulla are amines, such as epinephrine and norepinephrine.
What medicines are glucocorticoids?
Examples of glucocorticoid drugs include:
- beclomethasone.
- betamethasone.
- budesonide.
- cortisone.
- dexamethasone.
- hydrocortisone.
- methylprednisolone.
- prednisolone.
Are there any glucocorticoid receptor antagonists for psychosis?
Glucocorticoid Receptor Antagonists. GR antagonists counteract the effects of cortisol at tissue level by blocking the GR. At present, mifepristone is the only GR antagonist available for clinical use. Mifepristone has a rapid onset of action and can be useful in patients who present with acute complications, for example, psychosis,
Which is the best GR antagonist for cortisol?
GR antagonists counteract the effects of cortisol at tissue level by blocking the GR. At present, mifepristone is the only GR antagonist available for clinical use.
Can a GC antagonist be used as an exogenous corticosteroid?
All GC antagonists may produce adrenocortical insufficiency, which can be treated with exogenous corticosteroids such as hydrocortisone or dexamethasone. Hyperkalemia and hyponatremia should be identified and treated if necessary.
How does mifepristone work as a glucocorticoid antagonist?
Although mifepristone is a mixed glucocorticoid and progesterone antagonist, its effect on cognition, mood, affect and HPA regulation in animals and man are due to blockade of the GR. In summary, brain GR blockade interferes with the termination of the stress response.