Photoinduced Electron Transfer-Based Fluorescent Agonists for α1-Adrenergic Receptors Imaging
Xiaojun Qin1,2, Wenhua Li1, Xingye Yang1
1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250012, P. R. China.
Abstract:
The novel fluorescent agonists were discovered herein for α1-adrenergic receptors (α1-ARs) based on photoinduced electron transfer (PeT) off-on switch by conjugating the fluorophore 7-(diethylamino)coumarin-3-carboxylic acid with phenylephrine. After careful evaluation, these probes exhibited efficient binding affinity with α1-ARs and could be applied to selectively imaging α1-ARs or successfully tracing the dynamic process of α1-AR internalization in living cells. Meanwhile, a bioluminescence resonance energy transfer binding assay with these new probes has been well-established and applied. Therefore, these PeT-based on-off agonists may serve as powerful tools for the α1-AR-associated study during drug discovery.
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