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: 29122-68-7

Selleck's Atenolol has been cited by 2 publications

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

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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 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NCT01361087 Withdrawn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 Inc.
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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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