Synthesis and antidepressant-like activity of novel alkoxy-piperidine derivatives targeting SSRI/5-HT1A/5-HT7
Synthesis and antidepressant-like activity of novel alkoxy-piperidine derivatives targeting SSRI/5-HT1A/5-HT7
复制标题
靶向SSRI/5-HT1A/5-HT7的新型烷氧基哌啶衍生物的合成及其抗抑郁样活性
DOI：
10.1016/j.bmcl.2019.126769
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发表时间：
2019
影响因子：
2.7
通讯作者：
Li Jian-Qi
中科院分区：
文献类型：
--
作者：
Wang Wen-Tao;Qian Hao;Wu Jian-Wei;Chen Xiao-Wen;Li Jian-Qi
合成了一系列新的烷氧基哌啶衍生物，并评价了它们对5-HT1A/5- ht7受体的5-羟色胺再摄取抑制和结合亲和力。采用小鼠强迫游泳实验（FST）和悬尾实验（TST）探讨了选择性化合物的体内抗抑郁活性。结果表明，化合物7a（再摄取抑制（RUI））， IC50= 177 nM；5-HT1A Ki = 12 海里;5-HT7, Ki= 25 nM)和15g（RUI, IC50= 85 nM; 5-HT1A, Ki= 17 nM; 5-HT7, Ki= 35 nM）是动物行为模型中潜在的抗抑郁药物，具有5-HT1A/5-HT7受体高亲和力和适度的血清素再摄取抑制作用，体外代谢稳定性好。
A series of novel alkoxy-piperidine derivatives were synthesized and evaluated for their serotonin reuptake inhibitory and binding affinities for 5-HT1A/5-HT7receptors.In vivoantidepressant activities of the selective compounds were explored using the forced swimming test (FST) and tail suspension test (TST) in mice. The results showed that compounds7a(reuptake inhibition (RUI), IC50= 177 nM; 5-HT1A, Ki= 12 nM; 5-HT7, Ki= 25 nM) and15g(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-HT7receptor affinities and moderate serotonin reuptake inhibition, and good metabolic stabilityin vitro.