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Bepridil

Name: Bepridil
Description: A long-acting calcium-blocking agent 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. (PubChem) 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. Mechanism of action: 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 in vitro, 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. Drug type: Approved. Small Molecule. Drug category: Anti-Arrhythmia Agents. Antiarrhythmic Agents. Antihypertensive Agents. Calcium Channel Blockers. Vasodilator Agents
Synonym(s): Bepadin, Vascor
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB01244
Id: CHEBI_3061
Related to: Sodium channel protein type 5 subunit alpha, Voltage-dependent P/Q-type calcium channel subunit alpha-1A, Calmodulin, Potassium voltage-gated channel subfamily KQT member 1, Sodium/potassium-transporting ATPase alpha-1 chain, Troponin C, slow skeletal and cardiac muscles
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Commenttaken from DrugBank
CurationStatusuncurated  +
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB01244  +
DefinitionA long-acting calcium-blocking agent with A long-acting calcium-blocking agent 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. (PubChem) 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. Mechanism of action: 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 in vitro, 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. Drug type: Approved. Small Molecule. Drug category: Anti-Arrhythmia Agents. Antiarrhythmic Agents. Antihypertensive Agents. Calcium Channel Blockers. Vasodilator Agents lcium Channel Blockers. Vasodilator Agents
Has roleDrug  +
IdCHEBI_3061  +
LabelBepridil  +
ModifiedDate14 April 2014  +
RelatedToSodium channel protein type 5 subunit alpha  +, Voltage-dependent P/Q-type calcium channel subunit alpha-1A  +, Calmodulin  +, Potassium voltage-gated channel subfamily KQT member 1  +, Sodium/potassium-transporting ATPase alpha-1 chain  +, Troponin C  +, and Slow skeletal and cardiac muscles  +
SuperCategoryMolecular entity  +
SynonymBepadin  +, and Vascor  +