Synthesis and antidepressant effect of novel aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7
Synthesis and antidepressant effect of novel aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7
复制标题
靶向SSRI/5-HT1A/5-HT7的新型芳烷基哌嗪及哌啶衍生物的合成及抗抑郁作用
DOI：
10.1016/j.bmcl.2019.126703
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发表时间：
2019-12-01
影响因子：
2.7
通讯作者：
Li, Jian-Qi
中科院分区：
文献类型：
--
作者：
Gu, Zheng-Song;Wang, Wen-Tao;Li, Jian-Qi
合成了一系列新型芳烷基哌嗪和哌啶类化合物，并对它们的5-羟色胺再摄取抑制活性和5-HT1A/5-HT7受体亲和力进行了评价。采用强迫游泳实验(FST)和悬尾实验(TST)对该选择性化合物的体内抗抑郁活性进行了筛选。结果表明，化合物19a对5-羟色胺(1a/)5-HT7受体(5-HT1a，K-I=12 nM；5-HT7，Ki=3.2 nM)有较高的亲和力，并对5-羟色胺再摄取有很强的抑制作用(IC50=14 nM)，在FST和TST模型中表现出明显的抗抑郁药样作用。
A series of novel aralkyl piperazine and piperidine derivatives were synthesized, and evaluated for their serotonin reuptake inhibitory and 5-HT1A/5-HT7 receptors affinities activity. Antidepressant activities in vivo of the selective compound were screened using the forced swimming test (FST) and tail suspension test (TST). The results indicated that compound 19a exhibited high affinities for the 5-HT(1A/)5-HT7 receptors (5-HT1A, K-i = 12 nM; 5-HT7, Ki = 3.2 nM) coupled with potent serotonin reuptake inhibition (IC50 = 14 nM) and showed a marked antidepressant-like effect in the FST and TST models.