alprenolol indications/contra

Stem definitionDrug idCAS RN
beta-adrenoreceptor antagonists 137 13655-52-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alprenolol
  • alpheprol
  • dl-Alprenolol
  • (RS)-Alprenolol
  • (+/-)-Alprenolol
  • alprenoxime hydrochloride
  • alprenolol hydrochloride
  • alprenoxime HCl
  • alprenolol HCl
One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.
  • Molecular weight: 249.35
  • Formula: C15H23NO2
  • CLOGP: 2.65
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 2
  • TPSA: 41.49
  • ALOGS: -3.12
  • ROTB: 8

Drug dosage:

DoseUnitRoute
0.40 g O
0.40 g P

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1966 YEAR INTRODUCED

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC C07AA01 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Beta blocking agents, non-selective
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
MeSH PA D000889 Anti-Arrhythmia Agents
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35530 beta-adrenergic antagonist
CHEBI has role CHEBI:66991 sympatholytic agent
MeSH PA D000959 Antihypertensive Agents
MeSH PA D001337 Autonomic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D013565 Sympatholytics

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-2 adrenergic receptor GPCR ANTAGONIST Kd 9.66 SCIENTIFIC LITERATURE IUPHAR
Beta-1 adrenergic receptor GPCR ANTAGONIST Kd 9.68 SCIENTIFIC LITERATURE KEGG DRUG
5-hydroxytryptamine receptor 2A GPCR Ki 5.29 PDSP
Beta-3 adrenergic receptor GPCR Kd 6.86 CHEMBL
Squalene synthase Enzyme IC50 5.38 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 6.93 CHEMBL
Beta-2 adrenergic receptor GPCR IC50 8.53 CHEMBL

External reference:

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IDSource
563 IUPHAR_LIGAND_ID
N0000166828 NUI
C0002334 UMLSCUI
D01182 KEGG_DRUG
CHEMBL266195 ChEMBL_ID
2502C2OIRK UNII
13707-88-5 SECONDARY_CAS_RN
DB00866 DRUGBANK_ID
2119 PUBCHEM_CID
597 RXNORM
96294004 SNOMEDCT_US
N0000166828 NDFRT
005225 NDDF
2461 INN_ID
CHEBI:51211 CHEBI
CHEMBL1256179 ChEMBL_ID
CHEMBL2448147 ChEMBL_ID
D000526 MESH_DESCRIPTOR_UI
JTZ PDB_CHEM_ID

Pharmaceutical products:

None