Aralkyl and aralkylidene heterocyclic lactams and imides
申请人:——
公开号:US20020049214A1
公开(公告)日:2002-04-25
The present invention relates to compounds of the formula I
1
wherein R
1
, R
2
, R
3
, X, Y and the dashed line are as defined in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use as psychotherapeutic agents.
Neuroleptic activity of chiral trans-hexahydro-.gamma.-carbolines
作者:Reinhard Sarges、Harry R. Howard、Kathy M. Donahue、Williard M. Welch、Beryl W. Dominy、Albert Weissman、B. Kenneth Koe、Jon Bordner
DOI:10.1021/jm00151a002
日期:1986.1
A series of trans-8-fluoro-5-(4-fluorophenyl)-2,3,4,4a,5, 9b-hexahydro-1H-pyrido[4,3-b]indoles with various N-2 substituents has been prepared and tested for neuroleptic activity [( 3H]spiroperidol binding and amphetamine antagonism). Several members of this series showed exceptional in vivo potency, especially the hydantoin derivatives 27-30. Resolution into the enantiomers showed that neuroleptic activity is associated with the 4aS,9bS absolute configuration. These rigid neuroleptics have been correlated with other rigid neuroleptics [(+)-dexclamol, Ro 22-1319] and can serve to further define the topography of the dopamine receptor.