标题：Discovery of naphthalimide conjugates as fluorescent probes for alpha(1)-adrenoceptors
作者：Zhang, Wei; Zhou, Xin-Yang; Yu, Qin-Ying; Du, Lu-Pei; Li, Min-Yong
作者机构：[Zhang Wei] Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Key Laboratory of Chemical Biology (MOE), Jinan, Shandong 2500 更多
通讯作者地址：[Li, MY]Shandong Univ, Dept Med Chem, Key Lab Chem Biol MOE, Sch Pharm, Jinan 250012, Peoples R China.
关键词：alpha(1)-Adrenergic receptors; Fluorescent probes; High affinity; Cell; imaging
摘要：alpha(1)-Adrenoceptors (alpha(1)-ARs), including at least three subtypes, alpha(1A), alpha(1B) and alpha(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 napthalienide-based small-molecule fluorescent probes (1a -1f) for alpha(1)-ARs, including two parts, a pharmacophore (quinazoline and phenylpiperazine) for alpha(1)-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 alpha(1)-aradrenoceptors. (c) 2016 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.