Abstract

Fluorescent ligands have emerged as powerful tools for noninvasive research of G protein-coupled receptors (GPCRs), since they could provide the invaluable information regarding GPCRs' structure and function in vitro. However, the in vivo applications of thus tools are hampered owing to their short-wavelength spectra and lack of fluorogenic switch. Here, we describe the experimental details of discovery of the environment-sensitive near-infrared (NIR) fluorogenic ligand for in vivo imaging of α1-adrenergic receptor (α1-AR).

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