384803-50-3Relevant academic research and scientific papers
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.
A new efficient synthesis of 3-(4-pyridinyl)methylindoles
Zhou, Ping,Li, Yanfang,Meagher, Kristin L,Mewshaw, Richard G,Harrison, Boyd L
, p. 7333 - 7335 (2001)
A new efficient method for the preparation of 3-(4-pyridinyl)methylindoles has been developed. The new method involves coupling of indoles with 4-pyridinecarboxaldehyde to give 3-indolyl 4-pyridinyl methanols, which upon treatment with triethylsilane in the presence of trifluoroacetic acid afford 3-(4-pyridinyl)methylindoles in 64-76% overall yield.
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.
Heterocyclylalkylindole or -azaindole compounds as 5-hydroxytryptamine-6 ligands
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, (2008/06/13)
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
