|
|||||
|
|
Advances Toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT(1A) receptor antagonism/SSRI activities. Part 2 |
|
| Authors: | Takeuchi Kumiko Kohn Todd J Honigschmidt Nicholas A Rocco Vincent P Spinazze Patrick G Koch Daniel J Atkinson Steven T Hertel Larry W Nelson David L Wainscott D Bradley Ahmad Laura J Shaw Janice Threlkeld Penny G Wong David T |
| Institution: | Lilly Research Laboratories, A Division of Eli Lilly and Company, IN 46285, Indianapolis, USA. ktak@lilly.com |
| Abstract: | Potent 5-HT1A/SSRIs at low nanomolar and subnanomolar concentrations were identified in a series of 1-(1H-indol-4-yloxy)-3-(4-benzob]thiophen-2-ylpiperidinyl)propan-2-ols. Incorporation of an alpha-Me group in the piperidine ring with its specific stereochemistry enhanced binding affinity at the 5-HT reuptake site and in vitro 5-HT(1A) antagonist functional activity. |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ | |