Citation: Wei Zhang, Xin-Yang Zhou, Qin-Ying Yu, Lu-Pei Du, Min-Yong Li. Discovery of naphthalimide conjugates as fluorescent probes for α1-adrenoceptors[J]. Chinese Chemical Letters, ;2016, 27(02): 185-189. doi: 10.1016/j.cclet.2015.12.002 shu

Discovery of naphthalimide conjugates as fluorescent probes for α1-adrenoceptors

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Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan 250012, China

Corresponding author: Min-Yong Li,
Received Date: 25 July 2015
Available Online: 30 September 2015
Fund Project: The present work was supported by grants from the Fok Ying Tong Education Foundation (No. 122036) (No. 122036) the Program of New Century Excellent Talents in University (No. NCET-11-0306) (No. NCET-11-0306)the Independent Innovation Foundation of Shandong University, ⅡFSDU (No. 2010JQ005). Our cell imaging work was performed at the Microscopy Characterization Facility, Shandong University. We also thank Professor You-Yi Zhang from Peking University for her generous gift, the α_1A-AR-and α_1D-AR-transfected HEK293A cells. (No. JQ201019)

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-Adrenergic receptors,
- Fluorescent probes,
- High affinity,
- Cell imaging
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沈阳化工大学材料科学与工程学院沈阳 110142