dezocine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
847 53648-55-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dezocine hydrobromide
  • dalgan
  • dezocine
potent analgesic; RN given refers to ((5R-(5alpha,11alpha,13S*)))-isomer (dezocin); structure
  • Molecular weight: 245.37
  • Formula: C16H23NO
  • CLOGP: 3.72
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 2
  • TPSA: 46.25
  • ALOGS: -4.24
  • ROTB: 0

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 20 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.68 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 5.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 27.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.08 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
None FDA ASTRAZENECA

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 N02AX03 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Other opioids
MeSH PA D000700 Analgesics
MeSH PA D000701 Analgesics, Opioid
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D009294 Narcotics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:35482 narcotic analgesic

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

DiseaseRelationSNOMED_IDDOID
Pain indication 22253000




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.25 acidic
pKa2 9.39 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
Mu-type opioid receptor GPCR PARTIAL AGONIST EC50 7.42 CHEMBL CHEMBL
Kappa-type opioid receptor GPCR ANTAGONIST WOMBAT-PK CHEMBL

External reference:

IDSource
4019515 VUID
N0000147635 NUI
D00838 KEGG_DRUG
216364 RXNORM
4019515 VANDF
C0057626 UMLSCUI
CHEBI:4474 CHEBI
CHEMBL1685 ChEMBL_ID
DB01209 DRUGBANK_ID
C010827 MESH_SUPPLEMENTAL_RECORD_UI
3033053 PUBCHEM_CID
3906 INN_ID
VHX8K5SV4X UNII
4570 MMSL
534 MMSL
d00837 MMSL
003545 NDDF
108377005 SNOMEDCT_US
370233009 SNOMEDCT_US

Pharmaceutical products:

None