Atenolol

Catalog No.S4817 Synonyms: Tenormin, Normiten, Blokium

Atenolol Chemical Structure

Molecular Weight(MW): 266.34

Atenolol 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.

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Biological Activity

Description Atenolol 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

Animal Research:

[2]

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

Solubility (25°C)

In vitro DMSO 53 mg/mL (198.99 mM)
Ethanol 53 mg/mL (198.99 mM)
Water 35 mg/mL (131.41 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 266.34
Formula

C14H22N2O3

CAS No. 29122-68-7
Storage powder
in solvent
Synonyms Tenormin, Normiten, Blokium

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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NCT01361087 Withdrawn Other: Blood draw Marfan Syndrome Ann & Robert H Lurie Children''s Hospital of Chicago|Johns Hopkins University April 2011 Phase 3
NCT01522950 Completed Drug: Nebivolol|Drug: atenolol|Drug: placebo Hypertension University of Minnesota - Clinical and Translational Science Institute|Forest Laboratories May 2010 Phase 2
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

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Adrenergic Receptor Signaling Pathway Map

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