Photoinduced Electron Transfer-Based Fluorescent Agonists for α 1 -Adrenergic Receptors Imaging

The novel fluorescent agonists were discovered herein for α -adrenergic receptors (α -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 α -ARs and could be applied to selectively imaging α -ARs or successfully tracing the dynamic process of α -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 α -AR-associated study during drug discovery.