Title of article :
Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives Original Research Article
Author/Authors :
Dahui Zhou، نويسنده , , Ping Zhou، نويسنده , , Deborah A. Evrard، نويسنده , , Kristin Meagher، نويسنده , , Michael Webb، نويسنده , , Boyd L. Harrison، نويسنده , , Donna M. Huryn، نويسنده , , Jeannette Golembieski، نويسنده , , Geoffrey A. Hornby، نويسنده , , Lee E. Schechter، نويسنده , , Deborah L. Smith، نويسنده , , Terrance H. Andree، نويسنده , , Richard E. Mewshaw، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Pages :
17
From page :
6707
To page :
6723
Abstract :
Based on the previously reported discovery lead, 3-(cis-4-(4-(1H-indol-4-yl)piperazin-1-yl)cyclohexyl)-5-fluoro-1H-indole (2), a series of related arylpiperazin-4-yl-cyclohexyl indole analogs were synthesized then evaluated as 5-HT transporter inhibitors and 5-HT1A receptor antagonists. The investigation of the structure–activity relationships revealed the optimal pharmacophoric elements required for activities in this series. The best example from this study, 5-(piperazin-1-yl)quinoline analog (trans-20), exhibited equal binding affinities at 5-HT transporter (Ki = 4.9 nM), 5-HT1A receptor (Ki = 6.2 nM) and functioned as a 5-HT1A receptor antagonist.
Keywords :
5-HT1A receptor , Serotonin transporter
Journal title :
Bioorganic and Medicinal Chemistry
Serial Year :
2008
Journal title :
Bioorganic and Medicinal Chemistry
Record number :
1304477
Link To Document :
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