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

Stem definitionDrug idCAS RN
calcium channel blockers, verapamil derivatives 1275 16662-47-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • gallopamil
  • methoxyverapamil
  • gallopamil hydrochloride
  • gallopamil HCl
Coronary vasodilator that is an analog of iproveratril (VERAPAMIL) with one more methoxy group on the benzene ring.
  • Molecular weight: 484.64
  • Formula: C28H40N2O5
  • CLOGP: 4.01
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 0
  • TPSA: 73.18
  • ALOGS: -4.95
  • ROTB: 14

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1.75 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 14.30 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.07 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.80 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 19 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 48
kinase-selectivity-class AKT3,AXL,BRAF,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,IRAK3,PDK4,PIK3CD,PRKDC,SIK2,TEK,TTK 15
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 1.875 High 0.88
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 0.88
rat-kpuu-brain Rat brain Kpuu 0.148 % High 0.88

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C08DA02 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH DIRECT CARDIAC EFFECTS
Phenylalkylamine 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
CHEBI has role CHEBI:65023 anti-asthmatic agent

Related Drugs by ATC class:

C08DA Phenylalkylamine derivatives 2 drugs
etripamilverapamil

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 8.91 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
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 5.44 CHEMBL

External reference:

IDSource
N0000166522 NUI
D08009 KEGG_DRUG
C0016986 UMLSCUI
CHEBI:34772 CHEBI
CHEMBL51149 ChEMBL_ID
CHEMBL523367 ChEMBL_ID
D005711 MESH_DESCRIPTOR_UI
DB12923 DRUGBANK_ID
4318 INN_ID
39WPC8JHR8 UNII
1234 PUBCHEM_CID
439837 RXNORM
004173 NDDF
004174 NDDF
703433005 SNOMEDCT_US
703434004 SNOMEDCT_US
CHEMBL1256940 ChEMBL_ID
16662-46-7 SECONDARY_CAS_RN

Pharmaceutical products:

None