Hirosada Sugihara

Selective β-adrenoceptor activities of tetrahydronaphthalene derivatives

Abstract Alpha - and beta -adrenoceptor activities of a group of tetralin derivatives prepared as fixed analogs of isoproterenol, adrenaline and noradrenaline were evaluated in vitro assays. All of the present compounds showed strong direct β-stimulating activity fairly selective for tracheal muscle. Activity of a trans isomer about the C(1)-C(2) bond was ten times higher than that of the cis isomer. None of the compounds tested had any practical α-adrenoceptor activity. Structure-activity interrelationships between the present series of compounds and some known adrenergic agonists are discussed.