Repositioning Candidate Details
| Candidate ID: | R0463 |
| Source ID: | DB01244 |
| Source Type: | approved; withdrawn |
| Compound Type: | small molecule |
| Compound Name: | Bepridil |
| Synonyms: | Bepadin; Bepridil |
| Molecular Formula: | C24H34N2O |
| SMILES: | CC(C)COCC(CN(CC1=CC=CC=C1)C1=CC=CC=C1)N1CCCC1 |
| Structure: |
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| DrugBank Description: | A long-acting, non selective, calcium channel blocker with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. It is no longer marketed in the United States, as it has been implicated in causing ventricular arrhythmias (ie. Torsade de pointes). |
| CAS Number: | 64706-54-3 |
| Molecular Weight: | 366.5396 |
| DrugBank Indication: | For the treatment of hypertension, and chronic stable angina (classic effort-associated angina). |
| DrugBank Pharmacology: | Bepridil is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It is not related chemically to other calcium channel blockers such as diltiazem hydrochloride, nifedipine and verapamil hydrochloride. |
| DrugBank MoA: | Bepridil has inhibitory effects on both the slow calcium (L-type) and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. Bepridil inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. This has been demonstrated in isolated myocardial and vascular smooth muscle preparations in which both the slope of the calcium dose response curve and the maximum calcium-induced inotropic response were significantly reduced by bepridil. In cardiac myocytes <i>in vitro</i>, bepridil was shown to be tightly bound to actin. Bepridil regularly reduces heart rate and arterial pressure at rest and at a given level of exercise by dilating peripheral arterioles and reducing total peripheral resistance (afterload) against which the heart works. |
| Targets: | Voltage-dependent P/Q-type calcium channel subunit alpha-1A inhibitor; Voltage-dependent T-type calcium channel subunit alpha-1H inhibitor; Voltage-dependent calcium channel subunit alpha-2/delta-2 inhibitor; Sodium/potassium-transporting ATPase subunit alpha-1 inhibitor; Potassium voltage-gated channel subfamily KQT member 1 inhibitor; Troponin C, slow skeletal and cardiac muscles other; Calmodulin binder; Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B inhibitor; Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A inhibitor; Potassium voltage-gated channel subfamily H member 2 inhibitor |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S08 | Lifestyle measures | Lifestyle intervention; weight loss; diet adaptation; dietary interventions; lifestyle modifications; Exercise | -- | -- | Details |
| S11 | Anti-hypertensive | -- | angiotensin converting enzyme inhibitors (ACEi) ; angiotensin II receptor blockers (ARBs) | Captopril | Details |
| 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 |