STUDIES ON TETRAHYDROISOQUINOLINES (THI) (I) BRONCHODILATOR ACTIVITY AND STRUCTURE-ACTIVITY RELATIONSHIP

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Abstract
The bronchodilating action may be due to the B-sympathomimetic action, since the dose-response curves for THI were shifted to the higher concentration in the presence of pronethalol, as were those for epinephrine and isopro-terenol. The chemical structure essential for manifestation of the activity should include: 1,2,3,4-tetrahydroisoquinoline nucleus, 2 free hydroxyl groups at position 6 and 7, and arylmethyl group at position 1. l-(3,4,5-Trimethoxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrahy-droisoquinoline was about 10 times as active as isoproterenol. The possible structure of the B-receptor was discussed briefly.