Repositioning Candidate Details
| Candidate ID: | R0221 |
| Source ID: | DB00622 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Nicardipine |
| Synonyms: | Nicardipine |
| Molecular Formula: | C26H29N3O6 |
| SMILES: | COC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OCCN(C)CC1=CC=CC=C1 |
| Structure: |
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| DrugBank Description: | A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. |
| CAS Number: | 55985-32-5 |
| Molecular Weight: | 479.525 |
| DrugBank Indication: | Used for the management of patients with chronic stable angina and for the treatment of hypertension. |
| DrugBank Pharmacology: | Nicardipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nicardipine is similar to other peripheral vasodilators. Nicardipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload. |
| DrugBank MoA: | By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload. |
| Targets: | Voltage-dependent L-type calcium channel subunit alpha-1C inhibitor; Voltage-dependent L-type calcium channel subunit beta-2 inhibitor; Voltage-dependent calcium channel subunit alpha-2/delta-1 inhibitor; Voltage-dependent L-type calcium channel subunit alpha-1D inhibitor; Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A inhibitor; Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B inhibitor; Alpha-1A adrenergic receptor antagonist; Alpha-1B adrenergic receptor antagonist; Alpha-1D adrenergic receptor antagonist; Muscarinic acetylcholine receptor M1 antagonist; Muscarinic acetylcholine receptor M2 antagonist; Muscarinic acetylcholine receptor M3 antagonist; Muscarinic acetylcholine receptor M4 antagonist; Muscarinic acetylcholine receptor M5 antagonist; Calmodulin other/unknown |
| Inclusion Criteria: | Indication 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 | |
|---|---|---|---|---|---|
| I08 | 114 | Cardiovascular system disease | A disease of anatomical entity which occurs in the blood, heart, blood vessels or the lymphatic system that passes nutrients (such as amino acids and electrolytes), gases, hormones, blood cells or lymph to and from cells in the body to help fight diseases and help stabilize body temperature and pH to maintain homeostasis. http://en.wikipedia.org/wiki/Circulatory_system | disease of anatomical entity | Details |
| 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 |