74764-40-2

antineoplastic, alkylating agent

ChEBI: The hydrochloride monohydrate of bepridril.

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

Moderately toxic by ingestion.

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.

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%).

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

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

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