Repositioning Candidate Details
| Candidate ID: | R0206 |
| Source ID: | DB00594 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Amiloride |
| Synonyms: | 3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide; Amiloride; Amipramidin; Amipramidine; Amyloride; N-amidino-3,5-diamino-6-chloropyrazinecarboxamide |
| Molecular Formula: | C6H8ClN7O |
| SMILES: | NC(=N)NC(=O)C1=NC(Cl)=C(N)N=C1N |
| Structure: |
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| DrugBank Description: | A pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with diuretics to spare potassium loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705) |
| CAS Number: | 2609-46-3 |
| Molecular Weight: | 229.627 |
| DrugBank Indication: | For use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension. |
| DrugBank Pharmacology: | Amiloride, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is an antihypertensive, potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive heart failure. The drug is often used in conjunction with thiazide or loop diuretics. Due to its potassium-sparing capacities, hyperkalemia (high blood potassium levels) are occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements. |
| DrugBank MoA: | Amiloride works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone. |
| Targets: | Amiloride-sensitive sodium channel subunit alpha inhibitor; Amiloride-sensitive sodium channel subunit beta inhibitor; Amiloride-sensitive sodium channel subunit gamma inhibitor; Amiloride-sensitive sodium channel subunit delta inhibitor; Amiloride-sensitive amine oxidase [copper-containing] inhibitor; Acid-sensing ion channel 2 inhibitor; Acid-sensing ion channel 1 inhibitor; Sodium/hydrogen exchanger 1 inhibitor; Urokinase-type plasminogen activator 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 |