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

Stem definitionDrug idCAS RN
1014 77671-31-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fenoximone
  • enoximone
A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE.
  • Molecular weight: 248.30
  • Formula: C12H12N2O2S
  • CLOGP: 2.25
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 58.20
  • ALOGS: -3.56
  • ROTB: 3

Drug dosage:

DoseUnitRoute
1 g P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 96.65 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 1.48 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 19.10 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.30 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.94 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1988 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01CE03 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Phosphodiesterase inhibitors
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D058987 Phosphodiesterase 3 Inhibitors
MeSH PA D010726 Phosphodiesterase Inhibitors
MeSH PA D020011 Protective Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.41 acidic
pKa2 13.0 acidic

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
Phosphodiesterase 4 Enzyme IC50 5.54 CHEMBL
cGMP-inhibited 3',5'-cyclic phosphodiesterase A Enzyme IC50 5.34 WOMBAT-PK

External reference:

IDSource
N0000167073 NUI
C0116190 UMLSCUI
D04004 KEGG_DRUG
320067009 SNOMEDCT_US
49626 RXNORM
396042009 SNOMEDCT_US
003676 NDDF
C7Z4ITI7L7 UNII
5582 INN_ID
53708 PUBCHEM_CID
CHEBI:135010 CHEBI
CHEMBL249856 ChEMBL_ID
DB04880 DRUGBANK_ID
D017335 MESH_DESCRIPTOR_UI
9063 IUPHAR_LIGAND_ID

Pharmaceutical products:

None