384803-50-3Relevant articles and documents
Synthesis and antidepressant-like activity of novel alkoxy-piperidine derivatives targeting SSRI/5-HT1A/5-HT7
Chen, Xiao-Wen,Li, Jian-Qi,Qian, Hao,Wang, Wen-Tao,Wu, Jian-Wei
, (2019)
A series of novel alkoxy-piperidine derivatives were synthesized and evaluated for their serotonin reuptake inhibitory and binding affinities for 5-HT1A/5-HT7 receptors. In vivo antidepressant activities of the selective compounds were explored using the forced swimming test (FST) and tail suspension test (TST) in mice. The results showed that compounds 7a (reuptake inhibition (RUI), IC50 = 177 nM; 5-HT1A, Ki = 12 nM; 5-HT7, Ki = 25 nM) and 15g (RUI, IC50 = 85 nM; 5-HT1A, Ki = 17 nM; 5-HT7, Ki = 35 nM) were potential antidepressant agents in animal behavioral models with high 5-HT1A/5-HT7 receptor affinities and moderate serotonin reuptake inhibition, and good metabolic stability in vitro.
Studies toward the discovery of the next generation of antidepressants. Part 2: Incorporating a 5-HT1A antagonist component into a class of serotonin reuptake inhibitors
Mewshaw, Richard E.,Meagher, Kristin L.,Zhou, Ping,Zhou, Dahui,Shi, Xiaojie,Scerni, Rosemary,Smith, Deborah,Schechter, Lee E.,Andree, Terrance H.
, p. 307 - 310 (2007/10/03)
The design and synthesis of a novel series of indole derivatives (9) having dual 5-HT transporter reuptake and 5-HT1A antagonist activity are described.