Chemistry:Bepridil

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Short description: Calcium channel blocker medication
Bepridil
Bepridil.svg
Clinical data
Trade namesVascor
AHFS/Drugs.comMonograph
MedlinePlusa699051
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration
Oral
ATC code
Pharmacokinetic data
BioavailabilityWell absorbed
Protein binding99%
MetabolismHepatic, CYP3A4-mediated
Elimination half-life42 hours
ExcretionRenal
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEBI
ChEMBL
Chemical and physical data
FormulaC24H34N2O
Molar mass366.549 g·mol−1
3D model (JSmol)
  (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. "Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967)". Molecular Pharmacology 48 (3): 540–549. September 1995. PMID 7565636. http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=7565636. 
  2. "Use of bepridil in combination with Ic antiarrhythmic agent in converting persistent atrial fibrillation to sinus rhythm". Circulation Journal 72 (5): 709–715. May 2008. doi:10.1253/circj.72.709. PMID 18441448. 
  3. "A screen of approved drugs and molecular probes identifies therapeutics with anti-Ebola virus activity". Science Translational Medicine 7 (290): 290ra89. June 2015. 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.". Washington Post. 4 June 2015. https://www.washingtonpost.com/news/to-your-health/wp/2015/06/03/zoloft-as-ebola-cure-anti-depressant-is-one-of-a-number-of-promising-drugs-being-looked-at-by-scientists/. 
  5. "Bepridil is potent against SARS-CoV-2 in vitro". Proceedings of the National Academy of Sciences of the United States of America 118 (10): e2012201118. March 2021. doi:10.1073/pnas.2012201118. PMID 33597253. Bibcode2021PNAS..11812201V. 

External links