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ACS Med Chem Lett. 2015 Mar 30;6(5):502-6. doi: 10.1021/ml5004298. eCollection 2015 May 14.

Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.

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


α1-Adrenergic receptors (α1-ARs), as the essential members of G protein-coupled receptors (GPCRs), can mediate numerous physiological responses in the sympathetic nervous system. In the current research, a series of quinazoline-based small-molecule fluorescent probes to α1-ARs (1a-1e), including two parts, a pharmacophore for α1-AR recognition and a fluorophore for visualization, were well designed and synthesized. The biological evaluation results displayed that these probes held reasonable fluorescent properties, high affinity, accepted cell toxicity, and excellent subcellular localization imaging potential for α1-ARs.


cell imaging; fluorescent probes; quinazoline; subcellular localization; α1-Adrenergic receptors

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