nalorphine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists, morphinan derivates 1877 62-67-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nalorphine
  • allorphine
  • antorphine
  • lethidrone
  • N-Allylnormorphine
  • nalorphin
  • nalorphine hydrochloride
  • nalorphine HCl
A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.
  • Molecular weight: 311.38
  • Formula: C19H21NO3
  • CLOGP: 1.18
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 52.93
  • ALOGS: -2.36
  • ROTB: 2

Drug dosage:

None

ADMET properties:

None

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC V03AB02 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Antidotes
MeSH PA D002491 Central Nervous System Agents
MeSH PA D009292 Narcotic Antagonists
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.71 acidic
pKa2 7.88 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 Ki 9.42 CHEMBL
Delta-type opioid receptor GPCR Ki 6.92 CHEMBL
Mu-type opioid receptor GPCR Ki 9.72 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor IC50 7.32 CHEMBL
Kappa-type opioid receptor GPCR Ki 7.82 CHEMBL
Opioid receptor GPCR EC50 8.82 CHEMBL
Mu-type opioid receptor GPCR Ki 8.70 CHEMBL
Opioid receptor GPCR IC50 7.23 CHEMBL

External reference:

IDSource
D08247 KEGG_DRUG
6526001 SNOMEDCT_US
373774009 SNOMEDCT_US
004659 NDDF
9FPE56Z2TW UNII
57-29-4 SECONDARY_CAS_RN
CHEMBL415284 ChEMBL_ID
30 INN_ID
DB11490 DRUGBANK_ID
CHEBI:7458 CHEBI
5284595 PUBCHEM_CID
D009269 MESH_DESCRIPTOR_UI
CHEMBL1908349 ChEMBL_ID
1629 IUPHAR_LIGAND_ID

Pharmaceutical products:

None