Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors

BE Maryanoff, DF McComsey, GE Martin…

Index: Maryanoff, Bruce E.; McComsey, David F.; Martin, Gregory E.; Shank, Richard P. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 8 p. 983 - 988

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Citation Number: 8

Abstract

We synthesized 20 and 21 as conformationally constrained analogues of the dopamine receptor antagonist SKF-83742, as well as analogues 6–9, 16, and 18–22. Although 20 and 21 were inactive, 7, 9, and 19 showed strong binding to D-1, D-2, S-2, and α-1 receptors, as well as antipsychotic activity in vivo.