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fenoldopam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| dopaminergic agents dopamine derivatives used as cardiac stimulant/antihypertensives/diuretics | 1153 | 67227-56-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 6 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.50 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 41.50 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.12 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.27 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.010 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.590 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 2.698 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 10.789 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 37.490 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 32.620 | % | High | 1 |
| herg | hERG pIC50 | 4.855 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 18.793 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.890 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 37.440 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK2,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IGF1R,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK1,MAPK10,MAPK12,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MELK,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 | 71 | |||
| kinase-selectivity-class | ACVR2B,AXL,CDK9,DYRK1B,EIF2AK3,EPHB4,GRK2,MAP2K6,MAPK8,STK33,TEK,TGFBR1 | 12 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.825 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 134.276 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 43.420 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.524 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 47.700 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 45.499 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 83.620 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 33.030 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 586.138 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 23, 1997 | FDA | HOSPIRA |
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 | C01CA19 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES Adrenergic and dopaminergic agents |
| FDA MoA | N0000000117 | Dopamine Agonists |
| FDA EPC | N0000175580 | Dopaminergic Agonist |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35569 | α-adrenergic agonist |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:48561 | dopaminergic antagonist |
| CHEBI has role | CHEBI:51065 | dopamine agonist |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D015259 | Dopamine Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018491 | Dopamine Agonists |
Related Drugs by ATC class:
C01CA Adrenergic and dopaminergic agents 25 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Malignant essential hypertension | indication | 78975002 | DOID:10823 |
| Hypertensive urgency | indication | 443482000 | |
| Open-angle glaucoma | contraindication | 84494001 | DOID:1067 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.05 | acidic |
| pKa2 | 10.45 | acidic |
| pKa3 | 12.02 | acidic |
| pKa4 | 7.73 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| D(1A) dopamine receptor | GPCR | AGONIST | Kd | 7.55 | CHEMBL | CHEMBL | |||
| D(2) dopamine receptor | GPCR | Ki | 6.09 | CHEMBL | |||||
| D(1B) dopamine receptor | GPCR | Ki | 6.96 | PDSP | |||||
| D(4) dopamine receptor | GPCR | AGONIST | Ki | 6.50 | IUPHAR | ||||
| Lysine-specific demethylase 4E | Enzyme | Ki | 5.72 | CHEMBL | |||||
| Lysine-specific histone demethylase 1A | Enzyme | IC50 | 6.05 | CHEMBL | |||||
| Adrenergic receptor alpha-1 | GPCR | Kd | 5.30 | CHEMBL | |||||
| FAD-linked sulfhydryl oxidase ALR | Enzyme | AC50 | 5.86 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | Kd | 5.89 | CHEMBL | |||||
| D(1A) dopamine receptor | GPCR | Ki | 8.52 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | Ki | 6.10 | CHEMBL | |||||
| Adenosine A2b receptor | GPCR | Ki | 7.45 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021120 | VUID |
| N0000148574 | NUI |
| D00613 | KEGG_DRUG |
| 67287-54-1 | SECONDARY_CAS_RN |
| 67227-57-0 | SECONDARY_CAS_RN |
| 4021120 | VANDF |
| 4021121 | VANDF |
| C0060180 | UMLSCUI |
| CHEBI:5002 | CHEBI |
| CHEMBL588 | ChEMBL_ID |
| CHEMBL1026 | ChEMBL_ID |
| DB00800 | DRUGBANK_ID |
| D018818 | MESH_DESCRIPTOR_UI |
| 3341 | PUBCHEM_CID |
| 939 | IUPHAR_LIGAND_ID |
| 4673 | INN_ID |
| INU8H2KAWG | UNII |
| 155091 | RXNORM |
| 11504 | MMSL |
| 4719 | MMSL |
| 47924 | MMSL |
| d04257 | MMSL |
| 007356 | NDDF |
| 007357 | NDDF |
| 108590002 | SNOMEDCT_US |
| 108591003 | SNOMEDCT_US |
| 409138007 | SNOMEDCT_US |
| INU8H2KAWG | INXIGHT DRUGS |
Pharmaceutical products:
None