Repositioning Candidate Details
| Candidate ID: | R0144 |
| Source ID: | DB00414 |
| Source Type: | approved; investigational; withdrawn |
| Compound Type: | small molecule |
| Compound Name: | Acetohexamide |
| Synonyms: | 1-((p-Acetylphenyl)sulfonyl)-3-cyclohexylurea; 1-[(4-acetylbenzene)sulfonyl]-3-cyclohexylurea 4-acetyl-N-(cyclohexylcarbamoyl)benzenesulfonamide; Acetohexamide; N-(p-Acetylphenylsulfonyl)-N'-cyclohexylurea |
| Molecular Formula: | C15H20N2O4S |
| SMILES: | CC(=O)C1=CC=C(C=C1)S(=O)(=O)NC(=O)NC1CCCCC1 |
| Structure: |
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| DrugBank Description: | A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide. Acetohexamide has been discontinued in the US market. |
| CAS Number: | 968-81-0 |
| Molecular Weight: | 324.395 |
| DrugBank Indication: | Used in the management of diabetes mellitus type 2 (adult-onset). |
| DrugBank Pharmacology: | Acetohexamide is an intermediate-acting, first-generation oral sulfonylurea. It lowers blood sugar by stimulating the pancreatic beta cells to secrete insulin and by helping the body use insulin efficiently. Due to its primary action on the pancreatic beta cells, the drug is only effective when there are functional pancreatic beta cells that can produce insulin granules. Acetohexamide has one-third the potency of chlorpropamide, and twice the potency of tolbutamide; however, similar hypoglycemic efficacy occurs with equipotent dosage of sulfonylureas. |
| DrugBank MoA: | Sulfonylureas such as acetohexamide bind to an ATP-dependent K<sup>+</sup> channel on the cell membrane of pancreatic beta cells. This inhibits a tonic, hyperpolarizing outflux of potassium, which causes the electric potential over the membrane to become more positive. This depolarization opens voltage-gated Ca<sup>2+</sup> channels. The rise in intracellular calcium leads to increased fusion of insulin granulae with the cell membrane, and therefore increased secretion of (pro)insulin. |
| Targets: | ATP-sensitive inward rectifier potassium channel 1 inhibitor |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I05 | 9352 | Type 2 diabetes mellitus | A diabetes that is characterized by chronic hyperglycaemia with disturbances of carbohydrate, fat and protein metabolism resulting from defects in insulin secretion, insulin action, or both. A diabetes mellitus that is characterized by high blood sugar, insulin resistance, and relative lack of insulin. http://en.wikipedia.org/wiki/Diabetes, http://en.wikipedia.org/wiki/Diabetes_mellitus_type_2 | disease of metabolism/inherited metabolic disorder/ carbohydrate metabolic disorder/glucose metabolism disease/diabetes/ diabetes mellitus | Details |