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pargyline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| monoamine oxydase (MAO)-inhibitors type B | 2065 | 555-57-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A monoamine oxidase inhibitor with antihypertensive properties.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 39 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 | 2.283 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.212 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 42.170 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 94.842 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 38.140 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 28.760 | % | High | 1 |
| herg | hERG pIC50 | 4.517 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 42.073 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 50.350 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 37.060 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK | 42 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,DDR1,EPHB4,FLT3,GRK2,NUAK1,SIK2,TEK | 10 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.105 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 331.131 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 43.640 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.060 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 60.990 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 147.231 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 86.640 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 40.230 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 349.140 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1961 | FDA |
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 | C02KC01 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES OTHER ANTIHYPERTENSIVES MAO inhibitors |
| ATC | C02LL01 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION MAO inhibitors and diuretics |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D008996 | Monoamine Oxidase Inhibitors |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.84 | 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 | Ki | 5.74 | CHEMBL | CHEMBL | |||
| Amine oxidase [flavin-containing] A | Enzyme | INHIBITOR | IC50 | 5.47 | CHEMBL | CHEMBL | |||
| Amine oxidase [flavin-containing] B | Enzyme | Ki | 5.47 | CHEMBL | |||||
| Amine oxidase [flavin-containing] A | Enzyme | Ki | 5.07 | CHEMBL | |||||
| Aldehyde dehydrogenase, mitochondrial | Enzyme | IC50 | 5.25 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018734 | VUID |
| N0000179439 | NUI |
| D02564 | KEGG_DRUG |
| 306-07-0 | SECONDARY_CAS_RN |
| 4018734 | VANDF |
| 4019877 | VANDF |
| C0030557 | UMLSCUI |
| CHEBI:7930 | CHEBI |
| CHEMBL673 | ChEMBL_ID |
| DB01626 | DRUGBANK_ID |
| CHEMBL1200425 | ChEMBL_ID |
| D010293 | MESH_DESCRIPTOR_UI |
| 4688 | PUBCHEM_CID |
| 1350 | INN_ID |
| 7262 | IUPHAR_LIGAND_ID |
| 9MV14S8G3E | UNII |
| 7930 | RXNORM |
| 001497 | NDDF |
| 004598 | NDDF |
| 1536005 | SNOMEDCT_US |
| 21159006 | SNOMEDCT_US |
| 373749006 | SNOMEDCT_US |
| 9MV14S8G3E | INXIGHT DRUGS |
Pharmaceutical products:
None