bepridil Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
vasodilators 342 64706-54-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bepridil hydrochloride hydrate
  • bepridil hydrochloride
  • bepridil
  • dl-Bepridil
  • (+/-)-Bepridil
  • bepricol
  • Org 5730
  • bepridil monohydrochloride monohydrate
  • bepridil monohydrochloride
  • cordium
  • bepridil HCl
A long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist.
  • Molecular weight: 366.55
  • Formula: C24H34N2O
  • CLOGP: 6.20
  • LIPINSKI: 1
  • HAC: 3
  • HDO: 0
  • TPSA: 15.71
  • ALOGS: -4.75
  • ROTB: 10

Drug dosage:

DoseUnitRoute
0.30 g O

Approvals:

DateAgencyCompanyOrphan
Dec. 28, 1990 FDA

FDA Adverse Event Reporting System

None

Pharmacologic Action:

SourceCodeDescription
ATC C08EA02 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
NON-SELECTIVE CALCIUM CHANNEL BLOCKERS
Phenylalkylamine derivatives
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:35674 antihypertensive agent
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Angina pectoris indication 194828000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.79 Basic
pKa2 3.96 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Voltage-dependent L-type calcium channel subunit alpha-1D Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel BLOCKER Ki 5.15 WOMBAT-PK CHEMBL
Voltage-dependent P/Q-type calcium channel subunit alpha-1A Ion channel BLOCKER Ki 6.60 WOMBAT-PK
Potassium voltage-gated channel subfamily KQT member 4 Ion channel BLOCKER IC50 5 IUPHAR
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 Ion channel IC50 5.31 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.26 WOMBAT-PK
Sodium channel protein type 5 subunit alpha Ion channel WOMBAT-PK
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 6.08 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel IC50 4.66 CHEMBL
Lethal factor Enzyme IC50 5.32 CHEMBL
Potassium channel subfamily T member 1 Unclassified GATING INHIBITOR IC50 6 IUPHAR

External reference:

IDSource
4019549 VUID
N0000147653 NUI
C0770909 UMLSCUI
D00631 KEGG_DRUG
4W2P15D93M UNII
74764-40-2 SECONDARY_CAS_RN
3465 INN_ID
108530004 SNOMEDCT_US
4019631 VANDF
1436 RXNORM
372503006 SNOMEDCT_US
d00688 MMSL
004519 NDDF
CHEMBL1008 ChEMBL_ID
CHEMBL1200382 ChEMBL_ID
BEP PDB_CHEM_ID
CQN PDB_CHEM_ID
DB01244 DRUGBANK_ID
CHEBI:3061 CHEBI
2337 IUPHAR_LIGAND_ID
D015764 MESH_DESCRIPTOR_UI
2351 PUBCHEM_CID

Pharmaceutical products:

None