bepridil indications/contra

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:

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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 D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D014665 Vasodilator Agents
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:35674 antihypertensive agent

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Angina pectoris indication 194828000

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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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 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

External reference:

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IDSource
2337 IUPHAR_LIGAND_ID
4019549 VUID
N0000147653 NUI
C0770909 UMLSCUI
D00631 KEGG_DRUG
4W2P15D93M UNII
74764-40-2 SECONDARY_CAS_RN
3465 INN_ID
CHEMBL1008 ChEMBL_ID
4019631 VANDF
N0000006461 NDFRT
N0000147724 NDFRT
1436 RXNORM
108530004 SNOMEDCT_US
372503006 SNOMEDCT_US
d00688 MMSL
004519 NDDF
2351 PUBCHEM_CID
CHEMBL1200382 ChEMBL_ID
DB01244 DRUGBANK_ID
D015764 MESH_DESCRIPTOR_UI
CHEBI:3061 CHEBI
BEP PDB_CHEM_ID
CQN PDB_CHEM_ID

Pharmaceutical products:

None