Photoinduced Electron Transfer-Based Fluorescent Agonists for α1-Adrenergic Receptors Imaging

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.