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

Stem definitionDrug idCAS RN
beta-adrenoreceptor antagonists 569 56980-93-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • celiprolol
  • DL-Celiprolol
  • selectol
  • celiprolol hydrochloride
  • celiprolol HCl
  • celiprolol monohydrochloride
A cardioselective beta-1 adrenergic antagonist that has intrinsic symopathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.
  • Molecular weight: 379.50
  • Formula: C20H33N3O4
  • CLOGP: 1.86
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 90.90
  • ALOGS: -3.34
  • ROTB: 10

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 151 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 20 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 22.59 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 40 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1982 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C07AB08 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Beta blocking agents, selective
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D058671 Adrenergic beta-1 Receptor Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D013566 Sympathomimetics
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Angina pectoris indication 194828000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.38 acidic
pKa2 9.31 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-1 adrenergic receptor GPCR ANTAGONIST Ki 8.10 WOMBAT-PK SCIENTIFIC LITERATURE
Beta-2 adrenergic receptor GPCR AGONIST Ki 6.80 WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 5.05 CHEMBL

External reference:

IDSource
4025238 VUID
N0000171770 NUI
C0055021 UMLSCUI
D01741 KEGG_DRUG
349901006 SNOMEDCT_US
4025238 VANDF
003948 NDDF
20498 RXNORM
395960002 SNOMEDCT_US
CHEMBL27810 ChEMBL_ID
DRB57K47QC UNII
3979 INN_ID
57470-78-7 SECONDARY_CAS_RN
DB04846 DRUGBANK_ID
CHEBI:31385 CHEBI
9064 IUPHAR_LIGAND_ID
D017272 MESH_DESCRIPTOR_UI
CHEMBL1742424 ChEMBL_ID
2663 PUBCHEM_CID

Pharmaceutical products:

None