靶向α4β2 nAChR的戒烟药物的合成与生物活性评价  

Synthesis and Bioactivity Evaluation of Smoking Cessation Drugs Targeting α4β2 nAChR

作　　者：罗蒙强 张耀红[1] LUO Mengqiang;ZHANG Yaohong(School of Chemistry and Chemical Engineering,Shaoxing University,Shaoxing Zhejiang 312000)

机构地区：[1]绍兴文理学院化学化工学院,浙江绍兴312000

出　　处：《绍兴文理学院学报》2021年第10期38-46,共9页Journal of Shaoxing University

基　　金：浙江省自然科学基金项目“以nAChR为靶点的抗成瘾药物的结构改造与构效关系研究”(LQ16H090004).

摘　　要：烟草依赖是一种慢性成瘾性疾病,复发率高,严重威胁人类健康.以烟碱乙酰胆碱受体为作用靶点,设计合成14个环胍结构的化合物,首先对其进行放射性配体的竞争结合测试并进行构效关系分析,然后选择2个活性最好的化合物进行功能响应测试以及条件性位置偏爱测试,发现一个具有戒烟潜力的化合物13.Tobacco dependence,a chronic addictive disease with a high recurrence rate,seriously threatens human health.In this study,14 compounds with acyl guanidine structure targeting nicotinic acetylcholine receptors were designed and synthesized.Firstly,ligand binding assay was tested and the structure-activity relationship analysis was done.Then the two most active compounds were selected for function assay and conditioned place preference.Compound 13 was finally found to be a potential drug for smoking cessation.

关 键 词：烟草依赖 烟碱乙酰胆碱受体 戒烟药物 酰基环胍 

分 类 号：R971[医药卫生—药品]