Discovery of naphthalimide conjugates as fluorescent probes for α_1-adrenoceptors  

作　　者：Wei Zhang Xin-Yang Zhou Qin-Ying Yu Lu-Pei Du Min-Yong Li 

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

出　　处：《Chinese Chemical Letters》2016年第2期185-189,共5页中国化学快报（英文版）

基　　金：supported by grants from the Fok Ying Tong Education Foundation (No. 122036);the Program of New Century Excellent Talents in University (No. NCET-11-0306);the Shandong Natural Science Foundation (No. JQ201019);the Independent Innovation Foundation of Shandong University, IIFSDU (No. 2010JQ005)

摘　　要：α1-Adrenoceptors（α1-ARs）, including at least three subtypes, α（1A）, α（1B） and α（1D）, which play essential roles in G protein-coupled receptors（GPCRs）, can convey multiple pivotal extracellular signals in varied tissues and organs. In this research, a series of napthalimide-based small-molecule fluorescent probes（1a-1f） for α1-ARs, including two parts, a pharmacophore（quinazoline and phenylpiperazine） for α1-AR recognition and a fluorophore（naphthalimide） for visualization, were designed and synthesized successfully. These compounds display excellent fluorescence property and high affinity to receptors,which were used successfully for in vitro visualization of α1-adrenoceptors.α1-Adrenoceptors（α1-ARs）, including at least three subtypes, α（1A）, α（1B） and α（1D）, which play essential roles in G protein-coupled receptors（GPCRs）, can convey multiple pivotal extracellular signals in varied tissues and organs. In this research, a series of napthalimide-based small-molecule fluorescent probes（1a-1f） for α1-ARs, including two parts, a pharmacophore（quinazoline and phenylpiperazine） for α1-AR recognition and a fluorophore（naphthalimide） for visualization, were designed and synthesized successfully. These compounds display excellent fluorescence property and high affinity to receptors,which were used successfully for in vitro visualization of α1-adrenoceptors.

关 键 词：α1-Adrenergic receptors Fluorescent probes High affinity Cell imaging 

分 类 号：O657.3[理学—分析化学] TQ460.1[理学—化学]