Atenolol

Synonyms: Tenormin, Normiten, Blokium

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

Atenolol Chemical Structure

CAS No. 29122-68-7

Purity & Quality Control

Batch: S481701 DMSO]53 mg/mL]false]Ethanol]53 mg/mL]false]Water]35 mg/mL]false Purity: 99.88%
99.88

Atenolol Related Products

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 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].
Animal Research Animal Models spontaneously hypertensive rats (SHR), Wistar-Kyoto (WKY)
Dosages 20 mg/kg
Administration s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04224675 Unknown status
Aneurysm
Onassis Cardiac Surgery Centre
March 7 2020 Not Applicable
NCT01719367 Completed
Atrial Fibrillation
Vanderbilt University Medical Center
January 2013 Not Applicable
NCT01361087 Withdrawn
Marfan Syndrome
Ann & Robert H Lurie Children''s Hospital of Chicago|Johns Hopkins University
April 2011 Phase 3
NCT01132768 Terminated
Essential Hypertension|Carotid Plaque
Daiichi Sankyo Europe GmbH a Daiichi Sankyo Company|Daiichi Sankyo
May 2010 Phase 4

Chemical Information & Solubility

Molecular Weight 266.34 Formula

C14H22N2O3

CAS No. 29122-68-7 SDF --
Smiles CC(C)NCC(COC1=CC=C(C=C1)CC(=O)N)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 53 mg/mL ( (198.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 53 mg/mL

Water : 35 mg/mL


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In vivo
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