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 

作者机构：Department of Medicinal Chemistry Key Laboratory of Chemical Biology (MOE) School of Pharmacy Shandong University 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2016年第27卷第2期

页      面：185-189页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070302[理学-分析化学] 0703[理学-化学] 10[医学] 

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) 

主　　题：α1-Adrenergic receptors Fluorescent probes High affinity Cell imaging 

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.