Synthesis, binding affinity and selectivity of new β 1- and β 2-adrenoceptor blockers

The synthesis of a new series of sesamol derivatives with β-adrenergic blocking activity is described. The affinity and selectivity of these compounds for β 1- and β 2-adrenoceptors were studied in comparison with those of ICI-118551 and propranolol. Some of the synthesized compounds show very good...

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Bibliographic Details
Published in:Farmaco (Società chimica italiana : 1989) 1999-11, Vol.54 (11), p.713-720
Main Authors: Brizzi, Vittorio, Francioli, Marco, Brufani, Mario, Filocamo, Luigi, Bruni, Giancarlo, Massarelli, Paola
Format: Article
Language:English
Subjects:
Adrenergic beta-1 Receptor Antagonists
Adrenergic beta-2 Receptor Antagonists
Adrenergic beta-Antagonists - chemical synthesis
Adrenergic beta-Antagonists - metabolism
Adrenergic beta-Antagonists - pharmacology
Adrenoceptor blockers
Animals
Antihypertensive
Cardiovascular diseases
Lung - metabolism
Magnetic Resonance Spectroscopy
Male
Propanolamines - metabolism
Propanolamines - pharmacology
Protein Binding
Rats
Rats, Sprague-Dawley
Receptors, Adrenergic, beta-1 - metabolism
Receptors, Adrenergic, beta-2 - metabolism
Sesamol
Spectrophotometry, Infrared
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Summary:The synthesis of a new series of sesamol derivatives with β-adrenergic blocking activity is described. The affinity and selectivity of these compounds for β 1- and β 2-adrenoceptors were studied in comparison with those of ICI-118551 and propranolol. Some of the synthesized compounds show very good affinity for the β 2-receptors of rat lung membranes and two of them provide interesting selectivity.
ISSN:0014-827X
1879-0569
DOI:10.1016/S0014-827X(99)00077-4