AZEPINOINDOLE DERIVATIVES WITH HIGH-AFFINITY FOR BRAIN DOPAMINE AND SEROTONIN RECEPTORS

Authors
MARYANOFF BE MCCOMSEY DF MARTIN GE SHANK RP
Citation
Be. Maryanoff et al., AZEPINOINDOLE DERIVATIVES WITH HIGH-AFFINITY FOR BRAIN DOPAMINE AND SEROTONIN RECEPTORS, Bioorganic & medicinal chemistry letters, 8(8), 1998, pp. 983-988
Citations number
48
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
8
Year of publication
1998
Pages
983 - 988
Database
ISI
SICI code
0960-894X(1998)8:8<983:ADWHFB>2.0.ZU;2-U
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 s trong binding to D-l, D-2, S-2, and alpha-1 receptors, as well as anti psychotic activity in vivo. (C) 1998 Elsevier Science Ltd. All rights reserved.