Bepridil hydrochloride Property

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

WGK Germany 

2

RTECS 

UY1162000

Toxicity

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

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H317May cause an allergic skin reaction

H332Harmful if inhaled

H334May cause allergy or asthma symptoms or breathing difficulties if inhaled

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P271Use only outdoors or in a well-ventilated area.

P272Contaminated work clothing should not be allowed out of the workplace.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P285In case of inadequate ventilation wear respiratory protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P304+P341IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.

P342+P311IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician.

P363Wash contaminated clothing before reuse.

P501Dispose of contents/container to..…

Bepridil hydrochloride Chemical Properties,Usage,Production

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