Synthesis and antidepressant-like activity of novel alkoxy-piperidine derivatives targeting SSRI/5-HT(1A)/5-HT(7).
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Wang WT, Qian H, Wu JW, Chen XW, Li JQ
Synthesis and antidepressant-like activity of novel alkoxy-piperidine derivatives targeting SSRI/5-HT(1A)/5-HT(7).
Bioorg Med Chem Lett. 2019 Dec 15;29(24):126769. doi: 10.1016/j.bmcl.2019.126769. Epub 2019 Oct 28.
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- 31699607 [ View in PubMed]
- Abstract
A series of novel alkoxy-piperidine derivatives were synthesized and evaluated for their serotonin reuptake inhibitory and binding affinities for 5-HT(1A)/5-HT(7) 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), IC(50)=177nM; 5-HT(1A), K(i)=12nM; 5-HT(7), K(i)=25nM) and 15g (RUI, IC(50)=85nM; 5-HT(1A), K(i)=17nM; 5-HT(7), K(i)=35nM) were potential antidepressant agents in animal behavioral models with high 5-HT(1A)/5-HT(7) receptor affinities and moderate serotonin reuptake inhibition, and good metabolic stability in vitro.