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phenazocine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| narcotic antagonists/agonists related to 6,7-benzomorphan | 2119 | 127-35-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An opioid analgesic with actions and uses similar to MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1095)
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 3 | mg | P |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.286 | Moderate | 0.69 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.656 | Moderate | 0.69 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 30.479 | 10^-6 cm/s | Moderate | 0.69 |
| dh-clint | Dog hepatocyte intrinsic clearance | 46.132 | uL/min/10^6 cells | Moderate | 0.69 |
| dppb | Dog plasma protein binding (% unbound) | 9.700 | % | Moderate | 0.69 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 24.410 | % | Moderate | 0.69 |
| herg | hERG pIC50 | 5.803 | pIC50 | Moderate | 0.69 |
| hh-clint | Human hepatocyte intrinsic clearance | 36.141 | uL/min/10^6 cells | Moderate | 0.69 |
| hlm-clint | Human liver microsomal intrinsic clearance | 90.365 | uL/min/mg protein | Moderate | 0.69 |
| hppb | Human plasma protein binding (% unbound) | 9.050 | % | Moderate | 0.69 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 51 | |||
| kinase-selectivity-class | AXL,EIF2AK3,EPHB4,GRK2,MAP2K6,SIK2,TEK | 7 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.042 | Moderate | 0.69 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 162.181 | Moderate | 0.69 | |
| mppb | Mouse plasma protein binding (% unbound) | 11.580 | Moderate | 0.69 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.871 | Moderate | 0.69 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 22.750 | % | Moderate | 0.69 |
| rh-clint | Rat hepatocyte intrinsic clearance | 212.814 | uL/min/10^6 cells | Moderate | 0.69 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 42.230 | % | Moderate | 0.69 |
| rppb | Rat plasma protein binding (% unbound) | 9.760 | % | Moderate | 0.69 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 191.867 | uM | Moderate | 0.69 |
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:
| Source | Code | Description |
|---|---|---|
| ATC | N02AD02 | NERVOUS SYSTEM ANALGESICS OPIOIDS Benzomorphan derivatives |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000701 | Analgesics, Opioid |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D009294 | Narcotics |
| MeSH PA | D018689 | Sensory System Agents |
| CHEBI has role | CHEBI:35480 | analgesic |
Related Drugs by ATC class:
N02AD Benzomorphan derivatives 2 drugs
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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.26 | acidic |
| pKa2 | 9.16 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | Ki | 9.70 | CHEMBL | |||||
| Kappa-type opioid receptor | GPCR | Ki | 8.70 | CHEMBL | |||||
| Delta-type opioid receptor | GPCR | Ki | 8.30 | CHEMBL | |||||
| Mu-type opioid receptor | GPCR | IC50 | 8.10 | CHEMBL | |||||
| Mu-type opioid receptor | GPCR | IC50 | 8.01 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000166903 | NUI |
| 58073-76-0 | SECONDARY_CAS_RN |
| C0031376 | UMLSCUI |
| CHEBI:8056 | CHEBI |
| CHEMBL46399 | ChEMBL_ID |
| DB13606 | DRUGBANK_ID |
| CHEMBL2107297 | ChEMBL_ID |
| D010620 | MESH_DESCRIPTOR_UI |
| 14707 | PUBCHEM_CID |
| 900 | INN_ID |
| 1239-04-9 | SECONDARY_CAS_RN |
| J0ND6N0AQC | UNII |
| 104979 | RXNORM |
| 001564 | NDDF |
| 004626 | NDDF |
| 322619008 | SNOMEDCT_US |
| 387326002 | SNOMEDCT_US |
| 58360000 | SNOMEDCT_US |
Pharmaceutical products:
None