Brain bioluminolysis of a G protein-coupled receptor photodrug
Glòria Salort Flaquer, Marc López-Cano, Kenneth A. Jacobson, Francisco Ciruela · FENS Forum 2024
Photopharmacology is an emerging approach that allows the spatiotemporal control of receptor function using photodrugs and offers superior tissue specificity and reduced off-target effects. Previously, we successfully demonstrated the blockade the adenosine A2A receptor (A2AR) in mouse brain using MRS7145, a photocaged derivative of the selective A2AR antagonist SCH442416.1 Here, we explore the use of bioluminescence resonance energy transfer (BRET) to photouncage MRS7145 in vitro and in vivo. First, we demonstrated the effective release of SCH442416 by BRET uncaging or bioluminolysis of MRS71
ePoster · Neuroscience