Synthesis and renal vasodilator activity of some dopamine agonist 1-aryl-2, 3, 4, 5-tetrahydro-1H-3-benzazepine-7, 8-diols: halogen and methyl analogs of …

…, G Gallagher Jr, ME McCarthy, J Silvestri…

Index: Weinstock; Ladd; Wilson; Brush; Yim; Gallagher Jr.; McCarthy; Silvestri; Sarau; Flaim Journal of Medicinal Chemistry, 1986 , vol. 29, # 11 p. 2315 - 2325

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Citation Number: 50

Abstract

Certain 6-halo-l-phenyl-2, 3, 4, 5-tetrahydro-lH-3-benzazepines were found to be potent D-1 dopamine agonists. The 1-(4-hydroxyphenyl) analogues did not have central nervous system activity because their high polarity inhibited entry into the brain. However, these compounds were potent renal Vasodilators. Fenoldopam, the 6-chloro analogue, is an especially significant member of the series, and its synthesis, pharmacology, and clinical ...