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A series of 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline derivatives showed potent DA1 agonistic activities. We investigated the structure-activity relationship of the racemic compounds of this series. 4-(3,4-Dihydroxyphenyl)-7-methanesulfonamido-1,2,3,4-tetrahydroiso quinoline (43) was identified as a potent renal vasodilator with activity almost equal to that of YM435 (1).

4-(3,4-Dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline Derivatives. II. Their Renal Vasodilation Activity and Structure-Activity Relationship.