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Selective beta-adrenoceptor activities of tetrahydronaphthalene derivatives.
Authors:M Nishikawa  M Kanno  H Kuriki  H Sugihara  M Motohashi  K Itoh  O Miyashita  Y Oka  Y Sanno
Affiliation:Central Research Division, Takeda Chemical Industries, Ltd., Jusohonmachi, Yodogawa-ku, Osaka 532, Japan
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.
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