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

Stem definitionDrug idCAS RN
beta-adrenoreceptor antagonists 2027 6452-71-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • oxprenolol hydrochloride
  • oxprenolol
  • (+/-)-Oxprenolol
  • dl-Oxprenolol
  • oxprenolol HCl
A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.
  • Molecular weight: 265.35
  • Formula: C15H23NO3
  • CLOGP: 2.09
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 50.72
  • ALOGS: -2.59
  • ROTB: 9

  • Status: OFM

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

Drug dosage:

DoseUnitRoute
0.16 g O
0.16 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 30.86 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 3 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 15.14 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 44 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.72 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 7.70 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.19 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.09 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
None FDA NOVARTIS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C07AA02 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Beta blocking agents, non-selective
ATC C07BA02 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS AND THIAZIDES
Beta blocking agents, non-selective, and thiazides
ATC C07CA02 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS AND OTHER DIURETICS
Beta blocking agents, non-selective, and other diuretics
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
MeSH PA D014151 Anti-Anxiety Agents
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D013565 Sympatholytics
MeSH PA D014149 Tranquilizing Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Ventricular arrhythmia indication 44103008
Anxiety indication 48694002
Angina pectoris indication 194828000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.19 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
Beta-2 adrenergic receptor GPCR ANTAGONIST Ki 8 WOMBAT-PK CHEMBL
Beta-1 adrenergic receptor GPCR ANTAGONIST Ki 8.11 WOMBAT-PK CHEMBL
Solute carrier family 22 member 1 Transporter IC50 4.54 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 7.03 CHEMBL

External reference:

IDSource
C0700460 UMLSCUI
D01806 KEGG_DRUG
519MXN9YZR UNII
2506 INN_ID
96299009 SNOMEDCT_US
7801 RXNORM
387583006 SNOMEDCT_US
004748 NDDF
CHEBI:31949 CHEBI
CHEMBL546 ChEMBL_ID
CHEMBL1200745 ChEMBL_ID
6452-73-9 SECONDARY_CAS_RN
DB01580 DRUGBANK_ID
4631 PUBCHEM_CID
D010096 MESH_DESCRIPTOR_UI
7255 IUPHAR_LIGAND_ID

Pharmaceutical products:

None