Visualization of α_1-adrenergic receptors with phenylpiperazine-based fluorescent probes  

作　　者：Yuxing Lin Wenhua Li Qinying Yu Xinyang Zhou Wei Zhang Lupei Du Minyong Li 

机构地区：[1]Key Laboratory of Chemical Biology (Ministry of Education) [2]Department of Medicinal Chemistry, School of Pharmacy, Shandong University

出　　处：《Science China Chemistry》2016年第5期624-628,共5页中国科学（化学英文版）

基　　金：supported by the Fok Ying Tong Education Foundation (122036);the Program of New Century Excellent Talents in University (NCET-11-0306);the Major Project of Science and Technology of Shandong Province (2015ZDJS04001);the Shandong Natural Science Foundation (JQ201019);the Independent Innovation Foundation of Shandong University (2010JQ005)

摘　　要：Several novel fluorescent probes targeting α_1-adrenergic receptors were well designed and synthesized by conjugating phenylpiperazine pharmacophore with coumarin and fluorescein fluorophores. These compounds showed suitable fluorescence property, high receptor affinity, and low cytotoxicity. Moreover, the cell imaging results displayed that these probes can be effective tools for the real-time detection of ligand-receptor interactions, as well as the visualization and location of α_1-adrenergic receptors in living cells.Several novel fluorescent probes targetingα1-adrenergic receptors were well designed and synthesized by conjugating phenyl- piperazine pharmacophore with coumarin and fluorescein fluorophores. These compounds showed suitable fluorescence prop- erty, high receptor affinity, and low cytotoxicity. Moreover, the cell imaging results displayed that these probes can be effec- tive tools for the real-time detection of ligand-receptor interactions, as well as the visualization and location of α1-adrenergic receptors in living cells.

关 键 词：α1-adrenergic receptors fluorescent probes high affinity fluorescent imaging 

分 类 号：O657.3[理学—分析化学]