Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2017-11-06 , DOI: 10.1016/j.bmcl.2017.11.007 Zheng-Song Gu , Ying Xiao , Qing-Wei Zhang , Jian-Qi Li
A series of arylalkanol and aralkyl piperazine derivatives have been synthesized and evaluated for 5-HT reuptake inhibitory abilities and binding affinities at the 5-HT1A/5-HT7 receptors. Antidepressant activities of the compounds in vivo were screened using the forced swimming test (FST). The results indicated that the compound 8j exhibited high affinities for the 5-HT1A/5-HT7 receptors (5-HT1A, ki = 0.84 nM; 5-HT7, ki = 12 nM) coupling with moderate 5-HT reuptake inhibitory activity (RUI, IC50 = 100 nM) and showed a marked antidepressant-like activity in the FST model.
中文翻译:
一系列针对SSRI / 5-HT 1A / 5-HT 7的芳基链烷醇和芳烷基哌嗪衍生物的合成和抗抑郁活性
已经合成了一系列芳基链烷醇和芳烷基哌嗪衍生物,并评估了其对5-HT 1A / 5-HT 7受体的5-HT再摄取抑制能力和结合亲和力。使用强制游泳试验(FST)筛选了这些化合物在体内的抗抑郁活性。结果表明,化合物8j对5-HT 1A / 5-HT 7受体(5-HT 1A,k i = 0.84 nM; 5-HT 7,ki i = 12 nM)具有中等亲和力的高亲和力。HT再摄取抑制活性(RUI,IC 50 = 100 nM),并在FST模型中显示出明显的抗抑郁样活性。