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Article Abstract
A series of novel alkoxy-piperidine derivatives were synthesized and evaluated for their serotonin reuptake inhibitory and binding affinities for 5-HT/5-HT 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 = 177 nM; 5-HT, K = 12 nM; 5-HT, K = 25 nM) and 15g (RUI, IC = 85 nM; 5-HT, K = 17 nM; 5-HT, K = 35 nM) were potential antidepressant agents in animal behavioral models with high 5-HT/5-HT receptor affinities and moderate serotonin reuptake inhibition, and good metabolic stability in vitro.
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| http://dx.doi.org/10.1016/j.bmcl.2019.126769 | DOI Listing |
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Synthesis and antidepressant-like activity of novel alkoxy-piperidine derivatives targeting SSRI/5-HT/5-HT.
Bioorg Med Chem Lett
December 2019
Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, 285 Gebaini Road, Shanghai 201203, PR China. Electronic address:
A series of novel alkoxy-piperidine derivatives were synthesized and evaluated for their serotonin reuptake inhibitory and binding affinities for 5-HT/5-HT 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 = 177 nM; 5-HT, K = 12 nM; 5-HT, K = 25 nM) and 15g (RUI, IC = 85 nM; 5-HT, K = 17 nM; 5-HT, K = 35 nM) were potential antidepressant agents in animal behavioral models with high 5-HT/5-HT receptor affinities and moderate serotonin reuptake inhibition, and good metabolic stability in vitro.
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