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Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors
B E Maryanoff1, D F McComsey, G E Martin
1R. W. Johnson Pharmaceutical Research Institute, Spring House, Pennsylvania 19477, USA.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
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 alpha-1 receptors, as well as antipsychotic activity in vivo.