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Establishment of high throughput screening system of 5-HT_(1A) receptor agonists

文献类型：期刊论文

作者Sun Ying1; Cai Haiyan2; Shen Jingshan2; Zhu Weiliang2; Wang Heyao2; Guo Minliang1
刊名Chinese Pharmacological Bulletin
出版日期2012
卷号28期号:5页码:731-736
关键词Agonist HTS 5-HT_(1A) receptor depression endogeny stable cell line
ISSN号1001-1978
其他题名5-羟色胺1A受体激动剂高通量筛选模型的建立
文献子类Article
英文摘要Aim To discover 5-HT 1A receptor agonists,a high throughput screening system of 5-HT 1A receptor was established by detecting the activity of reporter gene.Methods The pcDNA3.1-h5-HT 1A R plasmid and pcDNA3.1-pCRE-luc plasmid which harbored a luciferase reporter gene were co-transfected into appropriate cells,and then assay conditions were studied and optimized,such as the chosen of cell lines,the ratio of plasmids,incubation time and positive compounds.Results ① According to the signal efficacy,HEK 293 cells were chosen.② To get the best signal-to-noise ratio(S/N),the plasmid ratio between pcDNA3.1-h5-HT 1A R and pcDNA3.1-pCRE-luc was 1:3 during the transient transfection experiment.③ The best incubation time of compound was 6 hours.④ As to positive compounds,5-HT.HCl,Flibanserin,8-OH-DPAT and Lorcaserin(APD356) were studied respectively.The result showed that APD356 should be the best positive compound for this screening system.⑤ The cell line was cultured for twelve generations,and the signal was stable.Conclusion In this study,a cell line that stably expresses 5-HT 1A receptor is built,assay conditions are studied and optimized,and finally,it is proved that the cell line is suitable for high throughput screening of 5-HT 1A receptor agonists.
资助项目国家科技重大专项《重大新药创制》课题[00000000] ; 上海市生物医药重点项目[00000000]
WOS研究方向General & Internal Medicine ; Neurosciences & Neurology ; Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种中文
CSCD记录号CSCD:4528860
源URL[http://119.78.100.183/handle/2S10ELR8/267858]  
专题药理学第三研究室
通讯作者Wang Heyao
作者单位1.College of Bioscience and Biotechnology,Yangzhou University, Yangzhou, Jiangsu 225009, China.;
2.Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China.
推荐引用方式
GB/T 7714		 Sun Ying,Cai Haiyan,Shen Jingshan,et al. Establishment of high throughput screening system of 5-HT_(1A) receptor agonists[J]. Chinese Pharmacological Bulletin,2012,28(5):731-736.
APA Sun Ying,Cai Haiyan,Shen Jingshan,Zhu Weiliang,Wang Heyao,&Guo Minliang.(2012).Establishment of high throughput screening system of 5-HT_(1A) receptor agonists.Chinese Pharmacological Bulletin,28(5),731-736.
MLA Sun Ying,et al."Establishment of high throughput screening system of 5-HT_(1A) receptor agonists".Chinese Pharmacological Bulletin 28.5(2012):731-736.

入库方式： OAI收割

来源：上海药物研究所

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