nalfurafine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists related to normorphine 4673 152657-84-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • TRK-820
  • winfuran
  • remitch
  • nalfurafine
  • nalfurafine hydrochloride
  • nalfurafine HCl
  • Molecular weight: 476.57
  • Formula: C28H32N2O5
  • CLOGP: 2.33
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 86.38
  • ALOGS: -3.47
  • ROTB: 5

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 21, 2009 PMDA

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 V03AX02 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Other therapeutic products

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

DiseaseRelationSNOMED_IDDOID
Severe Pruritus indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.64 acidic
pKa2 7.76 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
Kappa-type opioid receptor GPCR AGONIST Ki 9.64 CHEMBL SCIENTIFIC LITERATURE
Mu-type opioid receptor GPCR EC50 9.14 CHEMBL
Delta-type opioid receptor GPCR EC50 7.13 CHEMBL
Nociceptin receptor GPCR Ki 6.83 PDSP
Mitogen-activated protein kinase 3 Kinase EC50 9.26 CHEMBL
Mitogen-activated protein kinase 1 Kinase EC50 9.26 CHEMBL
Orexin receptor type 1 GPCR Ki 6.60 CHEMBL
Mu-type opioid receptor GPCR Ki 9.37 CHEMBL
Delta-type opioid receptor GPCR Ki 7.29 CHEMBL
Delta-type opioid receptor GPCR Ki 9.43 CHEMBL
Kappa-type opioid receptor GPCR Ki 9.75 CHEMBL
Kappa-type opioid receptor GPCR EC50 9.30 CHEMBL
Kappa-type opioid receptor GPCR Ki 9.75 CHEMBL
Mu-type opioid receptor GPCR Ki 9.24 CHEMBL

External reference:

IDSource
D06405 KEGG_DRUG
152658-17-8 SECONDARY_CAS_RN
CHEBI:136019 CHEBI
IVB PDB_CHEM_ID
CHEMBL267495 ChEMBL_ID
CHEMBL490665 ChEMBL_ID
CHEMBL485605 ChEMBL_ID
C111212 MESH_SUPPLEMENTAL_RECORD_UI
1651 IUPHAR_LIGAND_ID
8209 INN_ID
DB13471 DRUGBANK_ID
XC41AVD567 UNII
C2825264 UMLSCUI
6445230 PUBCHEM_CID

Pharmaceutical products:

None