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

Stem definitionDrug idCAS RN
neuromuscular blocking agents with rigid structure 3520 156137-99-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Org-9487
  • Org 9487
  • Org9487
  • rapacuronium bromide
  • raplon
  • rapacuronium
a nondepolarizing neuromuscular blocking agent with a rapid onset of action acts by competing for cholinergic receptors at the motor end plate
  • Molecular weight: 597.90
  • Formula: C37H61N2O4
  • CLOGP: 5.64
  • LIPINSKI: 2
  • HAC: 6
  • HDO: 0
  • TPSA: 55.84
  • ALOGS: -8.13
  • ROTB: 9
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.047 Moderate 0.72
caco2-efflux Caco-2 efflux ratio (BA/AB) 4.188 Moderate 0.72
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 16.293 10^-6 cm/s Moderate 0.72
dh-clint Dog hepatocyte intrinsic clearance 7.244 uL/min/10^6 cells Moderate 0.72
dppb Dog plasma protein binding (% unbound) 52.130 % Moderate 0.72
fcs-ppb Fetal calf serum protein binding (% unbound) 32.270 % Moderate 0.72
herg hERG pIC50 4.774 pIC50 Moderate 0.72
hh-clint Human hepatocyte intrinsic clearance 5.370 uL/min/10^6 cells Moderate 0.72
hlm-clint Human liver microsomal intrinsic clearance 26.792 uL/min/mg protein Moderate 0.72
hppb Human plasma protein binding (% unbound) 48.960 % Moderate 0.72
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,MAPKAPK2,NTRK2,PDK2,PDK4,PRKDC,TEK,TGFBR1 21
kinase-selectivity-class AXL,EIF2AK3,GRK2,MAP2K6 4
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 3.273 Moderate 0.72
mh-clint Mouse hepatocyte intrinsic clearance 81.470 Moderate 0.72
mppb Mouse plasma protein binding (% unbound) 41.390 Moderate 0.72
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 4.217 Moderate 0.72
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 52.590 % Moderate 0.72
rh-clint Rat hepatocyte intrinsic clearance 142.233 uL/min/10^6 cells Moderate 0.72
rh-fuinc Rat hepatocyte fraction unbound in incubation 79.100 % Moderate 0.72
rppb Rat plasma protein binding (% unbound) 48.450 % Moderate 0.72
solubility-dd Solubility at pH 7.4 in DMSO 968.278 uM Moderate 0.72

Approvals:

DateAgencyCompanyOrphan
Aug. 18, 1999 FDA ORGANON USA INC

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
MeSH PA D003473 Neuromuscular Nondepolarizing Agents
MeSH PA D009465 Neuromuscular Agents
MeSH PA D009466 Neuromuscular Blocking Agents
MeSH PA D018373 Peripheral Nervous System Agents

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

DiseaseRelationSNOMED_IDDOID
Muscle relaxation, function indication 11977004
General anesthesia indication 50697003
Skeletal Muscle Relaxation for Endotracheal Intubation indication
Skeletal Muscle Relaxation for Endotracheal Intubation in C-Section indication
Eaton-Lambert syndrome contraindication 56989000 DOID:0050214
Myasthenia gravis contraindication 91637004 DOID:437
Disease of liver contraindication 235856003 DOID:409




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.58 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
Muscle-type nicotinic acetylcholine receptor Ion channel ANTAGONIST CHEMBL SCIENTIFIC LITERATURE

External reference:

IDSource
4021207 VUID
N0000148653 NUI
D05703 KEGG_DRUG
465499-11-0 SECONDARY_CAS_RN
4021206 VANDF
4021207 VANDF
CHEMBL1201352 ChEMBL_ID
CHEMBL1200549 ChEMBL_ID
C082938 MESH_SUPPLEMENTAL_RECORD_UI
DB04834 DRUGBANK_ID
GG1LBM463S UNII
228530 RXNORM
31315 MMSL
8291 MMSL
d04450 MMSL
007881 NDDF
013422 NDDF
116106006 SNOMEDCT_US
763001001 SNOMEDCT_US
764600006 SNOMEDCT_US
C0876716 UMLSCUI
CHEBI:135845 CHEBI
5311399 PUBCHEM_CID
7635 INN_ID
GG1LBM463S INXIGHT DRUGS

Pharmaceutical products:

None