Repositioning Candidate Details
| Candidate ID: | R0301 |
| Source ID: | DB01011 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Metyrapone |
| Synonyms: | |
| Molecular Formula: | C14H14N2O |
| SMILES: | CC(C)(C(=O)C1=CN=CC=C1)C1=CC=CN=C1 |
| Structure: |
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| DrugBank Description: | An inhibitor of the enzyme steroid 11-beta-monooxygenase. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of cushing syndrome. |
| CAS Number: | 54-36-4 |
| Molecular Weight: | 226.2738 |
| DrugBank Indication: | Used as a diagnostic drug for testing hypothalamic-pituitary ACTH function. Occasionally used in Cushing's syndrome. |
| DrugBank Pharmacology: | Metopirone is an inhibitor of endogenous adrenal corticosteroid synthesis. |
| DrugBank MoA: | The pharmacological effect of Metopirone is to reduce cortisol and corticosterone production by inhibiting the 11-ß-hydroxylation reaction in the adrenal cortex. Removal of the strong inhibitory feedback mechanism exerted by cortisol results in an increase in adrenocorticotropic hormone (ACTH) production by the pituitary. With continued blockade of the enzymatic steps leading to production of cortisol and corticosterone, there is a marked increase in adrenocortical secretion of their immediate precursors, 11-desoxycortisol and desoxycorticosterone, which are weak suppressors of ACTH release, and a corresponding elevation of these steroids in the plasma and of their metabolites in the urine. These metabolites are readily determined by measuring urinary 17-hydroxycorticosteroids (17-OHCS) or 17-ketogenic steroids (17-KGS). Because of these actions, metopirone is used as a diagnostic test, with urinary 17-OHCS measured as an index of pituitary ACTH responsiveness. Metopirone may also suppress biosynthesis of aldosterone, resulting in a mild natriuresis. |
| Targets: | Cytochrome P450 11B1, mitochondrial; Camphor 5-monooxygenase |
| Inclusion Criteria: |
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