barnidipine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 290 104713-75-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • barnidipine
  • mepirodipine
  • vasexten
  • mepirodipine hydrobromide
  • mepirodipine hydrochloride
  • Molecular weight: 491.54
  • Formula: C27H29N3O6
  • CLOGP: 5.15
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 1
  • TPSA: 111.01
  • ALOGS: -5.09
  • ROTB: 9

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 1 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.357 Moderate 0.66
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.239 Moderate 0.66
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 12.050 10^-6 cm/s Moderate 0.66
dh-clint Dog hepatocyte intrinsic clearance 67.608 uL/min/10^6 cells Moderate 0.66
dppb Dog plasma protein binding (% unbound) 0.420 % Moderate 0.66
fcs-ppb Fetal calf serum protein binding (% unbound) 1 % Moderate 0.66
herg hERG pIC50 5.694 pIC50 Moderate 0.66
hh-clint Human hepatocyte intrinsic clearance 56.105 uL/min/10^6 cells Moderate 0.66
hlm-clint Human liver microsomal intrinsic clearance 272.898 uL/min/mg protein Moderate 0.66
hppb Human plasma protein binding (% unbound) 0.510 % Moderate 0.66
kinase-safety-class ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKDC,STK33,TEK,TTK,ZAP70 40
kinase-selectivity-class AXL,BRAF,CDK9,GRK2,STK33,TEK 6
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.780 Moderate 0.66
mh-clint Mouse hepatocyte intrinsic clearance 107.152 Moderate 0.66
mppb Mouse plasma protein binding (% unbound) 0.350 Moderate 0.66
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 13.490 Moderate 0.66
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 0.650 % Moderate 0.66
rh-clint Rat hepatocyte intrinsic clearance 139.316 uL/min/10^6 cells Moderate 0.66
rh-fuinc Rat hepatocyte fraction unbound in incubation 4.100 % Moderate 0.66
rppb Rat plasma protein binding (% unbound) 0.450 % Moderate 0.66
solubility-dd Solubility at pH 7.4 in DMSO 3.548 uM Moderate 0.66

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug interaction 69.53 47.23 41 636 500142 110088480
Hypomagnesaemia 52.55 47.23 18 659 60352 110528270

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C08CA12 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
CHEBI has role CHEBI:35554 cardiovascular drug

Related Drugs by ATC class:

C08CA Dihydropyridine derivatives 17 drugs
amlodipinebenidipinecelecoxibcilnidipineclevidipinefelodipineisradipinelacidipinelercanidipinelevamlodipinemanidipinenicardipine show all 17 →

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.17 Basic
pKa2 2.23 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-gated L-type calcium channel Ion channel BLOCKER DRUG LABEL KEGG DRUG

External reference:

IDSource
D07494 KEGG_DRUG
39879 RXNORM
C0078703 UMLSCUI
CHEBI:135793 CHEBI
CHEMBL2103761 ChEMBL_ID
DB09227 DRUGBANK_ID
6746 INN_ID
2VBY96ASWJ UNII
443869 PUBCHEM_CID
C050699 MESH_SUPPLEMENTAL_RECORD_UI
009143 NDDF
698052006 SNOMEDCT_US

Pharmaceutical products:

None