Photoinduced Electron Transfer-Based Fluorescent Agonists For Alpha(1)-Adrenergic Receptors Imaging

The novel fluorescent agonists were discovered herein for alpha(1)-adrenergic receptors (alpha(1)-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 alpha(1)-ARs and could be applied to selectively imaging alpha(1)-ARs or successfully tracing the dynamic process of alpha(1)-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 alpha(1)-AR-associated study during drug discovery.