Repositioning Candidate Details
| Candidate ID: | R0332 |
| Source ID: | DB01119 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Diazoxide |
| Synonyms: | |
| Molecular Formula: | C8H7ClN2O2S |
| SMILES: | CC1=NS(=O)(=O)C2=C(N1)C=CC(Cl)=C2 |
| Structure: |
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| DrugBank Description: | A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. |
| CAS Number: | 364-98-7 |
| Molecular Weight: | 230.671 |
| DrugBank Indication: | Used parentally to treat hypertensive emergencies. Also used to treat hypoglycemia secondary to insulinoma. |
| DrugBank Pharmacology: | Diazoxide is a potassium channel activator. Its mechanism of action revolves around enhancing cell membrane permeability to potassium ions. This action consequently elicits the relaxation of local smooth muscles. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential. |
| DrugBank MoA: | As a diuretic, diazoxide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like diazoxide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of diazoxide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. As a antihypoglycemic, diazoxide inhibits insulin release from the pancreas, probably by opening potassium channels in the beta cell membrane. |
| Targets: | ATP-sensitive inward rectifier potassium channel 11; NA |
| Inclusion Criteria: |
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