Repositioning Candidate Details
| Candidate ID: | R0491 |
| Source ID: | DB01325 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Quinethazone |
| Synonyms: | Quinethazon; Quinethazone |
| Molecular Formula: | C10H12ClN3O3S |
| SMILES: | CCC1NC(=O)C2=CC(=C(Cl)C=C2N1)S(N)(=O)=O |
| Structure: |
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| DrugBank Description: | Quinethazone, marketed as Hydromox, is a thiazide diuretic indicated for hypertension. Patients may experience adverse reactions such as dizziness, dry mouth, nausea, and hypokalemia. |
| CAS Number: | 73-49-4 |
| Molecular Weight: | 289.739 |
| DrugBank Indication: | Used to treat hypertension. |
| DrugBank Pharmacology: | Quinethazone is a thiazide diuretic used to treat hypertension. It inhibits Na<sup>+</sup>/Cl<sup>-</sup> reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue. |
| DrugBank MoA: | As a diuretic, quinethazone 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 quinethazone 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 quinethazone 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. |
| Targets: | Carbonic anhydrase 1 inhibitor; Carbonic anhydrase 2 inhibitor; Solute carrier family 12 member 1 inhibitor; Solute carrier family 12 member 2 inhibitor; Solute carrier family 12 member 3 inhibitor |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I12 | 10763 | Hypertension | An artery disease characterized by chronic elevated blood pressure in the arteries. https://en.wikipedia.org/wiki/Hypertension, https://www.ncbi.nlm.nih.gov/pubmed/24352797 | disease of anatomical entity/ cardiovascular system disease/vascular disease/ artery disease | Details |