Structure-activity relationships of substituted 2,3,4,4a,5,10b-hexahydro-benz[h]isoquinoline-6(1H)-ones as 5-HT2C receptor antagonists

Authors
Stadler, H Wichmann, J Sleight, AJ Bos, M
Citation
H. Stadler et al., Structure-activity relationships of substituted 2,3,4,4a,5,10b-hexahydro-benz[h]isoquinoline-6(1H)-ones as 5-HT2C receptor antagonists, CHIMIA, 54(11), 2000, pp. 669-671
Citations number
12
Categorie Soggetti
Chemistry
Journal title
CHIMIA
ISSN journal
00094293 → ACNP
Volume
54
Issue
11
Year of publication
2000
Pages
669 - 671
Database
ISI
SICI code
0009-4293(2000)54:11<669:SROS2>2.0.ZU;2-U
Abstract
A series of cis and trans configured 2,3,4,4a,5,10b-hexahydro-benz[h]isoqui noline-6(1H)-ones 2 were studied with respect to the binding affinity to th e 5-HT2 subtype receptors. The influence of substituents in positions 7 (R- 1), 8 (R-2) and 9 (R-3) on affinity and selectivity to 5-HT2A and 5-HT2C re ceptors and the preference of one diastereoisomer is discussed.