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Bepridil

From Wikipedia, the free encyclopedia
Calcium channel blocker medication
Pharmaceutical compound
Bepridil
Clinical data
Trade namesVascor
AHFS/Drugs.comMonograph
MedlinePlusa699051
Routes of
administration
Oral
ATC code
Pharmacokinetic data
BioavailabilityWell absorbed
Protein binding99%
MetabolismHepatic,CYP3A4-mediated
Eliminationhalf-life42 hours
ExcretionRenal
Identifiers
  • N-benzyl-N-(3-isobutoxy-2-pyrrolidin-1-yl-propyl)aniline
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC24H34N2O
Molar mass366.549 g·mol−1
3D model (JSmol)
  • O(CC(C)C)CC(N1CCCC1)CN(c2ccccc2)Cc3ccccc3
  • 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 nameVascor) is andiaminecalcium channel blocker once used to treatangina 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 ofatrial fibrillation.[2]

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

Ebola research

[edit]

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

SARS-CoV-2 research

[edit]

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

References

[edit]
  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)".Molecular Pharmacology.48 (3):540–549.doi:10.1016/S0026-895X(25)10504-X.PMID 7565636.
  2. ^Imai S, Saito F, Takase H, Enomoto M, Aoyama H, Yamaji S, et al. (May 2008)."Use of bepridil in combination with Ic antiarrhythmic agent in converting persistent atrial fibrillation to sinus rhythm".Circulation Journal.72 (5):709–715.doi:10.1253/circj.72.709.PMID 18441448.
  3. ^Johansen LM, DeWald LE, Shoemaker CJ, Hoffstrom BG, Lear-Rooney CM, Stossel A, et al. (June 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. ^Cha AE (4 June 2015)."Zoloft as Ebola cure? Antidepressant is one of a number of promising drugs being looked at by scientists".Washington Post.
  5. ^Vatansever EC, Yang KS, Drelich AK, Kratch KC, Cho CC, Kempaiah KR, et al. (March 2021)."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.Bibcode:2021PNAS..11812201V.doi:10.1073/pnas.2012201118.PMC 7958448.PMID 33597253.

External links

[edit]
Calcium
VDCCsTooltip Voltage-dependent calcium channels
Blockers
Activators
Potassium
VGKCsTooltip Voltage-gated potassium channels
Blockers
Activators
IRKsTooltip Inwardly rectifying potassium channel
Blockers
Activators
KCaTooltip Calcium-activated potassium channel
Blockers
Activators
K2PsTooltip Tandem pore domain potassium channel
Blockers
Activators
Sodium
VGSCsTooltip Voltage-gated sodium channels
Blockers
Activators
ENaCTooltip Epithelial sodium channel
Blockers
Activators
ASICsTooltip Acid-sensing ion channel
Blockers
Chloride
CaCCsTooltip Calcium-activated chloride channel
Blockers
Activators
CFTRTooltip Cystic fibrosis transmembrane conductance regulator
Blockers
Activators
Unsorted
Blockers
Others
TRPsTooltip Transient receptor potential channels
LGICsTooltip Ligand gated ion channels
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