Bepridil

Bepridil
Clinical data
Trade namesVascor
AHFS/Drugs.comMonograph
MedlinePlusa699051
Routes of
administration		Oral
ATC code
Pharmacokinetic data
BioavailabilityWell absorbed
Protein binding99%
MetabolismHepatic, CYP3A4-mediated
Elimination half-life42 hours
ExcretionRenal
Identifiers
IUPAC name
  • N-benzyl-N-(3-isobutoxy-2-pyrrolidin-1-yl-propyl)aniline
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H34N2O
Molar mass366.549 g·mol−1
3D model (JSmol)
SMILES
  • O(CC(C)C)CC(N1CCCC1)CN(c2ccccc2)Cc3ccccc3
InChI
  • InChI=1S/C24H34N2O/c1-21(2)19-27-20-24(25-15-9-10-16-25)18-26(23-13-7-4-8-14-23)17-22-11-5-3-6-12-22/h3-8,11-14,21,24H,9-10,15-20H2,1-2H3 checkY
  • Key:UIEATEWHFDRYRU-UHFFFAOYSA-N checkY
  (verify)

Bepridil (trade name Vascor) is an diamine calcium channel blocker once used to treat angina pectoris. It is no longer sold in the United States.

It is nonselective.[1]

It has been discussed as a possible option in the treatment of atrial fibrillation.[2]

It has been implicated in causing ventricular arrhythmia (torsades de pointes).

Ebola research

In June 2015 a research paper [3] was published finding bepridil to result in a 100% survival rate for mice exposed to ebola during an experiment searching for potential pharmaceutical ebola treatments; indicating its potential use in future ebola research and therapy.[4]

SARS-CoV-2 research

A research paper [5] showed that Bepridil inhibited cytopathogenic effects induced by SARS-CoV-2 in Vero E6 cells and in A549 cells in an in vitro assay.

References

  1. ↑ Bezprozvanny I, Tsien RW (September 1995). "Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967)". Mol. Pharmacol. 48 (3): 540–9. PMID 7565636.
  2. ↑ Imai S, Saito F, Takase H, et al. (May 2008). "Use of bepridil in combination with Ic antiarrhythmic agent in converting persistent atrial fibrillation to sinus rhythm". Circ. J. 72 (5): 709–15. doi:10.1253/circj.72.709. PMID 18441448.
  3. ↑ Johansen, Lisa M.; Dewald, Lisa Evans; Shoemaker, Charles J.; Hoffstrom, Benjamin G.; Lear-Rooney, Calli M.; Stossel, Andrea; Nelson, Elizabeth; Delos, Sue E.; Simmons, James A.; Grenier, Jill M.; Pierce, Laura T.; Pajouhesh, Hassan; Lehár, Joseph; Hensley, Lisa E.; Glass, Pamela J.; White, Judith M.; Olinger, Gene G. (2015). "A screen of approved drugs and molecular probes identifies therapeutics with anti–Ebola virus activity". Science Translational Medicine. 7 (290): 290ra89. doi:10.1126/scitranslmed.aaa5597. PMID 26041706.
  4. ↑ "Zoloft as Ebola cure? Antidepressant is one of a number of promising drugs being looked at by scientists".
  5. ↑ Erol CV, Kai Y, Kaci CK, Aleksandra D, Chia-Chuan C, Drake MM, Shiqing X, Chien-Te KT, Wenshe RL (March 2021). "Bepridil is potent against SARS-CoV-2 In Vitro". Proceedings of the National Academy of Sciences. 118 (10): e2012201118. doi:10.1073/pnas.2012201118. PMC 7958448. PMID 33597253.


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