Synthesis, Resolution, and Renal Vasodilation Activity of Novel DA_1 Agonists : 4-(3,4-Dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline Derivatives

概要

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7,8-Dihydroxy-4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline (1) and 4-(3,4-dihydroxyphenyl)-7-hydroxy-8-methyl-1,2,3,4-tetrahydroisoquinoline (2) are potent renal vasodilators which selectively stimulate DA_1 (peripheral dopamine receptor-1) receptors. Especially, (S)-(-)-1 is the most potent. Its DA_1 agonist activity is about 10 times stronger than dopamine for increasing renal blood flow in anesthetized dogs. The renal and cardiovascular effects of (S)-(-)-1 may be suitable for the treatment of patients with renal insufficiency, heart failure and hypertension.
公益社団法人日本薬学会の論文
1991-11-25