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  • Title: Bis-arenoxypropanolamines as potential beta-adrenolytics: a reinvestigation.
    Author: Da Re P, Valenti P, Fabbri G, Frigeni V, Reggiani A, Della Bella D.
    Journal: Drugs Exp Clin Res; 1988; 14(11):687-92. PubMed ID: 2907738.
    Abstract:
    A number of symmetrical as well as asymmetrical bis-arenoxypropanolamines have been synthesized and evaluated for their beta-adrenolytic properties. The pharmacological characterization of these compounds was performed in vitro by direct studies (3H-dihydroalprenolol was used as the specific ligand for beta-receptors), and by determining the beta-blocking capacity on isoproterenol (ISO)-induced increased heart rate (isolated guinea-pig atrium); and in vivo by evaluating the antagonism on ISO-induced hypotension and tachycardia, as well as the intrinsic sympathomimetic activity (ISA) on reserpinized and vagotomized rats. The best result was observed with the simplest derivative, i.e. the bis-phenoxypropanolamine compound, which shows in vitro and in vivo potencies almost comparable to propranolol and, moreover, significant bronchodilating activity.
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