Potency and selectivity in vitro of compounds related to isoprenaline and orciprenaline on beta-adrenoceptors in the guinea-pig

Abstract

1 Amines related in structure to either isoprenaline (catechol series) or orciprenaline (resorcinol series) were examined for activity on isolated trachea (relaxation), atria (chronotropic action) and perfused hind-limb (vasodilatation) of the guinea-pig.2 Compounds with a resorcinol nucleus were less potent on all three preparations but more selective for trachea than were compounds with a catechol nucleus.3 In both catechol and resorcinol compounds potency on trachea was enhanced by and selectivity for trachea was favoured by substitution of a p-OH phenyl group in the N-iso propyl, or by replacement of the N-iso propyl with an N-t-butyl, with or without a p-OH phenyl group.4 Most of the compounds, particularly the resorcinols, had much lower potencies, relative to isoprenaline, on hind-limb than on trachea.5 Some of the problems associated with the quantitative measurement of selectivity and with sub-classification of beta-adrenoceptors are discussed.