Synthesis and pharmacological characterization of 1-phenyl-, 4-phenyl-, and 1-benzyl-1, 2, 3, 4-tetrahydroisoquinolines as dopamine receptor ligands

…, JP Bowen, DL McDougald, RB Mailman

Index: Charifson; Wyrick; Hoffman; Ademe Simmons; Bowen; McDougald; Mailman Journal of Medicinal Chemistry, 1988 , vol. 31, # 10 p. 1941 - 1946

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Citation Number: 34

Abstract

A series of 1-phenyl-, 4-phenyl-, and 1-benzyl-1, 2, 3, 4-tetrahydroisoquinolines have been prepared as ring-contracted analogues of the prototypical D, dopamine receptor antagonist SCH23390 [(R)-(+)-7-chloro-8-hydroxy-3-methyll-pheny1-2, 3, 4, 5-tetrahydro-lH-3- benzazepine]. The affinity and selectivity of these isoquinolines for D1 receptors was determined by three biochemical endpoints in membrane homogenate5 prepared from rat ...