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  • Title: Cardioselective beta-adrenoceptor blocking actions of some 2-methoxyphenylethanolamines in guinea pig tissues.
    Author: Letts LG, Temple DM, Williams LR.
    Journal: Circ Res; 1980 Jun; 46(6 Pt 2):I51-2. PubMed ID: 6103760.
    Abstract:
    A series of new phenylethanolamines with 2-methoxy and/or 4-methyl, 4-chloro, or 4-bromo ring substituents and either N-isopropyl or N-tert butyl substituents have been synthesized and tested for beta 1- and beta 2-adrenoceptor blocking activity using isolated guinea pig atrial and tracheal preparations. Each of the disubstituted N-isopropyl derivatives was a potent antagonist, and the 2-methoxy-4-methyl derivative had a 40-fold beta 1/beta 2-receptor selectivity. Atenolol was shown to have a 32-fold selectivity in the same tests.
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