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

Stem definitionDrug idCAS RN
spasmolytics with a papaverine-like action 3025 479-81-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bietamiverine monohydrochloride
  • bietamiverine hydrochloride
  • bietamiverine
  • dietamiverine
  • novosaprol
  • paparid
  • spasmaparid
  • Molecular weight: 318.46
  • Formula: C19H30N2O2
  • CLOGP: 4.41
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 32.78
  • ALOGS: -3
  • ROTB: 9

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.549 Moderate 0.71
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.656 Moderate 0.71
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 27.290 10^-6 cm/s Moderate 0.71
dh-clint Dog hepatocyte intrinsic clearance 44.875 uL/min/10^6 cells Moderate 0.71
dppb Dog plasma protein binding (% unbound) 61.090 % Moderate 0.71
fcs-ppb Fetal calf serum protein binding (% unbound) 58.610 % Moderate 0.71
herg hERG pIC50 4.874 pIC50 Moderate 0.71
hh-clint Human hepatocyte intrinsic clearance 9.727 uL/min/10^6 cells Moderate 0.71
hlm-clint Human liver microsomal intrinsic clearance 48.084 uL/min/mg protein Moderate 0.71
hppb Human plasma protein binding (% unbound) 62.720 % Moderate 0.71
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.604 Moderate 0.71
mh-clint Mouse hepatocyte intrinsic clearance 255.859 Moderate 0.71
mppb Mouse plasma protein binding (% unbound) 68.230 Moderate 0.71
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.726 Moderate 0.71
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 81.570 % Moderate 0.71
rh-clint Rat hepatocyte intrinsic clearance 178.649 uL/min/10^6 cells Moderate 0.71
rh-fuinc Rat hepatocyte fraction unbound in incubation 85.960 % Moderate 0.71
rppb Rat plasma protein binding (% unbound) 61.860 % Moderate 0.71
solubility-dd Solubility at pH 7.4 in DMSO 843.335 uM Moderate 0.71

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:

None

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 9.19 Basic
pKa2 6.92 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
Muscarinic acetylcholine receptor M1 GPCR Ki 6.57 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 5.99 CHEMBL
Muscarinic acetylcholine receptor M3 GPCR Ki 6.73 CHEMBL

External reference:

IDSource
1477-10-7 SECONDARY_CAS_RN
C0602297 UMLSCUI
CHEBI:135362 CHEBI
CHEMBL2110892 ChEMBL_ID
CHEMBL2106541 ChEMBL_ID
C005680 MESH_SUPPLEMENTAL_RECORD_UI
72064 PUBCHEM_CID
669 INN_ID
4MGI916O6Y UNII

Pharmaceutical products:

None