Bepridil hydrochloride Chemical Properties

Melting point:

91 ±2°

storage temp. 

Desiccate at RT

solubility 

Soluble in DMSO (up to 25 mg/ml) or ethanol (up to 25 mg/ml)

form 

powder

color 

white

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.

Safety Information

WGK Germany 

2

RTECS 

UY1162000

Toxicity

LD50 in mice (mg/kg): 1955 orally, 23.5 i.v. (Mauvernay, 1978)

Bepridil hydrochloride Usage And Synthesis

Description

Bepridil (74764-40-2) is a clinically useful calcium channel blocker with antianginal activity.1 It has recently been shown to possess potent activity against SARS-CoV-2 in vitro.2 Bepridil was also able to provide protection from Ebola virus3 and other filoviruses in a mouse model4.

Uses

antineoplastic, alkylating agent

Uses

Bepridil Hydrochloride is a calcium channel blocker. It also activates mitochondrial ATP-sensitive KATP channelsBepridil Hydrochloride is an antiarrhythmic and antihypertensive agent and used for treating atrial fibrillation.

Definition

ChEBI: The hydrochloride monohydrate of bepridril.

brand name

Bepadin (Medpointe); Vascor (Johnson & Johnson).

General Description

Bepridil hydrochloride,β-[(2-methylpropoxy)methyl]-N-phenyl-N-(phenylmethyl)-1-pyrrolidineethylamine hydrochloride (Vascor), is a secondgenerationalkylamine-type channel blocker, structurallyunrelated to the dihydropyridines. Its actions are less specificthan those of the three prototypical channel blockers,verapamil, diltiazem, and nifedipine. In addition to being aCa²⁺ channel blocker, it inhibits sodium flow into the hearttissue and lengthens cardiac repolarization, causing bradycardia.Caution should be used if it is given to a patient withhypokalemia. Bepridil hydrochloride is used for stableangina. The drug has a half-life of 33 hours and is highlybound to protein (99%).

Hazard

Moderately toxic by ingestion.

Biochem/physiol Actions

Non-selective calcium channel blocker and class IV antiarrhythmic agent; inhibits Na+-Ca2+ exchange; inhibits growth of brain tumor cells in vitro.

Mechanism of action

In addition to class IV effects, bepridil also shows class I effects. The substance is active against both supraventricular and ventricular arrhythmias , .

References

Hollingshead et al. (1992), A review of its pharmacological properties and therapeutic use in stable angina pectoris; Drugs, 44 835 Vatansever et al. (2021), Bepridil is potent against SARS-CoV-2 in vitro; Proc. Natl. Acad. Sci USA, 118 e2012201118 Johansen et al. (2015), A screen of approved drugs and molecular probes identifies therapeutics with anti-Ebola virus activity; Sci. Transl. Med., 7 290ra89 DeWald et al. (2018), The calcium channel blocker bepridil demonstrates efficacy in the murine model of marburg virus disease; J. Infect. Dis., 218(suppl 5) S588

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