fenoldopam Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
dopaminergic agents dopamine derivatives used as cardiac stimulant/antihypertensives/diuretics 1153 67227-56-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fenoldopam hydrobromide
  • fenoldopam
  • fenoldopam mesylate
  • corlopam
  • fenoldopam mesilate
A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.
  • Molecular weight: 305.76
  • Formula: C16H16ClNO3
  • CLOGP: 2.40
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 4
  • TPSA: 72.72
  • ALOGS: -3.05
  • ROTB: 1

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
Sept. 23, 1997 FDA HOSPIRA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01CA19 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Adrenergic and dopaminergic agents
FDA EPC N0000175580 Dopaminergic Agonist
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:35569 alpha-adrenergic agonist
CHEBI has role CHEBI:51065 dopamine agonist
CHEBI has role CHEBI:35674 antihypertensive agent
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018491 Dopamine Agonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Malignant essential hypertension indication 78975002 DOID:10823
Hypertensive urgency indication 443482000
Open-angle glaucoma contraindication 84494001 DOID:1067

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(1A) dopamine receptor GPCR AGONIST Kd 7.55 CHEMBL CHEMBL
D(4) dopamine receptor GPCR AGONIST Ki 6.50 IUPHAR
D(2) dopamine receptor GPCR Ki 6.09 CHEMBL
Lysine-specific demethylase 4E Enzyme Ki 5.72 CHEMBL
Adrenergic receptor alpha-1 GPCR Kd 5.30 CHEMBL
FAD-linked sulfhydryl oxidase ALR Enzyme AC50 5.86 CHEMBL
D(1B) dopamine receptor GPCR Ki 6.96 PDSP
D(2) dopamine receptor GPCR Ki 6.10 CHEMBL
D(1A) dopamine receptor GPCR Ki 8.52 CHEMBL
D(2) dopamine receptor GPCR Kd 5.89 CHEMBL
Adenosine A2b receptor GPCR Ki 7.45 CHEMBL

External reference:

IDSource
4021120 VUID
N0000148574 NUI
C0060180 UMLSCUI
D00613 KEGG_DRUG
2BQI8R8GEM UNII
67287-54-1 SECONDARY_CAS_RN
409138007 SNOMEDCT_US
4021120 VANDF
24853 RXNORM
108590002 SNOMEDCT_US
47924 MMSL
d04257 MMSL
007356 NDDF
CHEBI:5002 CHEBI
CHEMBL588 ChEMBL_ID
CHEMBL1026 ChEMBL_ID
DB00800 DRUGBANK_ID
4673 INN_ID
3341 PUBCHEM_CID
D018818 MESH_DESCRIPTOR_UI
939 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Corlopam HUMAN PRESCRIPTION DRUG LABEL 1 0409-2304 INJECTION, SOLUTION 10 mg INTRAVENOUS NDA 15 sections
Corlopam HUMAN PRESCRIPTION DRUG LABEL 1 0409-3373 INJECTION, SOLUTION 10 mg INTRAVENOUS NDA 15 sections