Topic: adenosine A2A receptor

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

Cannabidiol (CBD) is a phytocannabinoid with potential as a therapy for a variety of diseases. CBD may act via cannabinoid receptors but also via other G-protein-coupled receptors (GPCRs), including the adenosine A2A receptor. Homogenous binding and signaling assays in Chinese hamster ovary (CHO) cells expressing the human version of the A2A receptor were performed to address the effect of CBD on receptor functionality. CBD was not able to compete for the binding of a SCH 442416 derivative labeled with a red emitting fluorescent probe that is a selective antagonist that binds to the orthosteri