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olprinone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| cardiac stimulants, amrinone derivatives | 1987 | 106730-54-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 0.64 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 11 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.13 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.618 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 33.189 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 3.334 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.055 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 64.900 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 76.560 | % | High | 1 |
| herg | hERG pIC50 | 4.245 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.140 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.034 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 56.580 | % | High | 1 |
| kinase-safety-class | ACVR1B,ACVR2A,ACVR2B,ALK,AURKA,AURKB,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,CHEK1,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,GSK3B,HASPIN,IKBKB,IRAK1,ITK,JAK1,KIT,MAP3K10,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK7,MAPK9,MARK4,MET,MTOR,NTRK1,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TNIK,TTK,ULK1,ULK2 | 62 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,CAMK2D,CDK9,DYRK1B,EIF2AK3,GRK2,MAPK7,MARK4,PRKDC,SIK2,STK33 | 13 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.690 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 2.972 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 62.940 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 6.546 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 68.930 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.349 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 88.190 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 49.600 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 44.361 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 1, 1996 | PMDA |
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 |
|---|---|---|
| MeSH PA | D002316 | Cardiotonic Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D010726 | Phosphodiesterase Inhibitors |
| MeSH PA | D020011 | Protective Agents |
| MeSH PA | D058987 | Phosphodiesterase 3 Inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute heart failure | indication | 56675007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.71 | acidic |
| pKa2 | 5.31 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Phosphodiesterase 3 | Enzyme | INHIBITOR | DRUG LABEL | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| D02042 | KEGG_DRUG |
| 119615-63-3 | SECONDARY_CAS_RN |
| C0637063 | UMLSCUI |
| CHEBI:135019 | CHEBI |
| CHEMBL1474900 | ChEMBL_ID |
| DB16847 | DRUGBANK_ID |
| C059498 | MESH_SUPPLEMENTAL_RECORD_UI |
| 4593 | PUBCHEM_CID |
| 7123 | INN_ID |
| 4Y8BMI9YGC | UNII |
Pharmaceutical products:
None