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Synthesis, binding affinity and selectivity of new beta 1- and beta 2-adrenoceptor blockers
V Brizzi1, M Francioli, M Brufani
1Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Italy. brizzi@unisi.it
Abstract:
The synthesis of a new series of sesamol derivatives with beta-adrenergic blocking activity is described. The affinity and selectivity of these compounds for beta 1- and beta 2-adrenoceptors were studied in comparison with those of ICI-118551 and propranolol. Some of the synthesized compounds show very good affinity for the beta 2-receptors of rat lung membranes and two of them provide interesting selectivity.