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aminophenazone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-inflammatory analgesics, phenylbutazone derivatives | 171 | 58-15-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A pyrazolone with analgesic, anti-inflammatory, and antipyretic properties but has risk of AGRANULOCYTOSIS. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of CYTOCHROME P-450 metabolic activity in LIVER FUNCTION TESTS.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.50 | g | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 55.55 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 247.05 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 100 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.852 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.603 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 58.614 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 14.997 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 86.210 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 87.350 | % | High | 1 |
| herg | hERG pIC50 | 3.948 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.084 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.246 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 83.400 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K21,MAPK7,NTRK2,PDK2,PDK4,PIK3CB,PRKDC,STK33,TEK | 22 | |||
| kinase-selectivity-class | ACVR2B,AXL,GRK2,MAPK7,STK33 | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.382 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 48.306 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 83.460 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.619 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 91.080 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 13.002 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 96.850 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 80.220 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 924.698 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1964 | YEAR INTRODUCED |
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 | N02BB03 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Pyrazolones |
| ATC | N02BB53 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Pyrazolones |
| ATC | N02BB73 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Pyrazolones |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory drug |
| CHEBI has role | CHEBI:35481 | non-narcotic analgesic |
| CHEBI has role | CHEBI:35493 | antipyretic |
| CHEBI has role | CHEBI:35703 | xenobiotic |
| CHEBI has role | CHEBI:78298 | environmental contaminant |
Related Drugs by ATC class:
N02BB Pyrazolones 4 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 | 5.06 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 2 | Enzyme | WOMBAT-PK | |||||||
| Prostaglandin G/H synthase 1 | Enzyme | WOMBAT-PK | |||||||
| Nicotinate phosphoribosyltransferase | Enzyme | Ki | 9 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000167058 | NUI |
| D00556 | KEGG_DRUG |
| 695 | RXNORM |
| C0002586 | UMLSCUI |
| CHEBI:160246 | CHEBI |
| CHEMBL288470 | ChEMBL_ID |
| DB01424 | DRUGBANK_ID |
| 6009 | PUBCHEM_CID |
| 375 | INN_ID |
| 01704YP3MO | UNII |
| D000632 | MESH_DESCRIPTOR_UI |
| D000983 | MESH_DESCRIPTOR_UI |
| 001608 | NDDF |
| 65458000 | SNOMEDCT_US |
Pharmaceutical products:
None