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iproniazid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1480 | 54-92-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An irreversible inhibitor of monoamine oxidase types A and B that is used as an antidepressive agent. It has also been used as an antitubercular agent, but its use is limited by its toxicity.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 35 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.595 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.005 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 33.037 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.350 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 90.180 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 91.680 | % | High | 1 |
| herg | hERG pIC50 | 3.489 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.167 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 2.877 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 94.430 | % | High | 1 |
| kinase-safety-class | ACVR2A,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,ITK,MAP3K21,MAP3K7,MAPK12,MAPK7,MARK4,NTRK2,PDK2,PDK4,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 31 | |||
| kinase-selectivity-class | AXL,BRAF,CAMK2D,CDK9,DYRK1B,EPHB4,ERBB2,GRK2,SIK2 | 9 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.773 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.035 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 94.750 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.311 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 96.470 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.563 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 96.720 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 92.720 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 959.401 | uM | High | 1 |
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 | N06AF05 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Monoamine oxidase inhibitors, non-selective |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D008996 | Monoamine Oxidase Inhibitors |
| MeSH PA | D011619 | Psychotropic Drugs |
| CHEBI has role | CHEBI:35469 | antidepressant |
Related Drugs by ATC class:
N06AF Monoamine oxidase inhibitors, non-selective 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Depressive disorder | indication | 35489007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.67 | acidic |
| pKa2 | 3.65 | Basic |
| pKa3 | 0.76 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Amine oxidase [flavin-containing] B | Enzyme | INHIBITOR | IC50 | 5.12 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Amine oxidase [flavin-containing] A | Enzyme | INHIBITOR | IC50 | 5.18 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Amine oxidase [flavin-containing] B | Enzyme | IC50 | 5.12 | CHEMBL | |||||
| Amine oxidase [flavin-containing] A | Enzyme | IC50 | 5.30 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000167316 | NUI |
| D02579 | KEGG_DRUG |
| 305-33-9 | SECONDARY_CAS_RN |
| C0022059 | UMLSCUI |
| CHEBI:5958 | CHEBI |
| CHEMBL92401 | ChEMBL_ID |
| DB04818 | DRUGBANK_ID |
| CHEMBL1256361 | ChEMBL_ID |
| D007490 | MESH_DESCRIPTOR_UI |
| 3748 | PUBCHEM_CID |
| 19 | INN_ID |
| D892HFI3XA | UNII |
| 353560 | RXNORM |
| 005260 | NDDF |
| 005261 | NDDF |
| 1217172005 | SNOMEDCT_US |
| 387438007 | SNOMEDCT_US |
| 76962009 | SNOMEDCT_US |
| D892HFI3XA | INXIGHT DRUGS |
Pharmaceutical products:
None