Atenolol

Catalog No.S4817 Synonyms: Tenormin, Normiten, Blokium

For research use only.

Atenolol (Tenormin, Normiten, Blokium) is a selective β1 receptor antagonist with log Kd values of −6.66±0.05, −5.99±0.14, −4.11±0.07 for binding to the human β1-, β2- and β3-adrenoceptors.

Atenolol Chemical Structure

CAS No. 29122-68-7

Selleck's Atenolol has been cited by 1 Publication

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Biological Activity

Description Atenolol (Tenormin, Normiten, Blokium) is a selective β1 receptor antagonist with log Kd values of −6.66±0.05, −5.99±0.14, −4.11±0.07 for binding to the human β1-, β2- and β3-adrenoceptors.
Targets
β1 receptor [1]
(Cell-free assay)
β2 receptor [1]
(Cell-free assay)
0.25 μM(Kd) 1 μM(Kd)
In vivo In clinical pharmacokinetics studies, atenolol is a hydrophilic betareceptor blocking drug, which is predominantly eliminated via the kidneys, only about 5% of the atenolol is metabolised by the liver. After oral administration atenolol is incompletely absorbed from the intestine, so about 50% of the beta blocker are finally biovailable. In plasma only 3% of atenolol are protein-bound. After oral administration elimination half life of atenolol is calculated from 6 to 9 h. There exists a linear relationship between the atenolol plasma levels and the degree of beta blocking effect measured by inhibition of the exercise-induced tachycardia while no correlation is found between plasma levels of atenolol and blood pressure lowering activity of the drug[3].

Protocol (from reference)

Animal Research:

[2]

  • Animal Models: spontaneously hypertensive rats (SHR), Wistar-Kyoto (WKY)
  • Dosages: 20 mg/kg
  • Administration: s.c.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 266.34
Formula

C14H22N2O3

CAS No. 29122-68-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)NCC(COC1=CC=C(C=C1)CC(=O)N)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04224675 Not yet recruiting Drug: Atenolol Aneurysm Onassis Cardiac Surgery Centre March 7 2020 Not Applicable
NCT01719367 Completed Drug: Atenolol Atrial Fibrillation Vanderbilt University Medical Center January 2013 Not Applicable
NCT01361087 Withdrawn Other: Blood draw Marfan Syndrome Ann & Robert H Lurie Children''s Hospital of Chicago|Johns Hopkins University April 2011 Phase 3
NCT01132768 Terminated Drug: Atenolol|Drug: olmesartan medoxomil Essential Hypertension|Carotid Plaque Daiichi Sankyo Europe GmbH a Daiichi Sankyo Company|Daiichi Sankyo Inc. May 2010 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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