Remote control of movement disorders using a photoactive adenosine A_2A receptor antagonist.

ABSTRACT: G protein-coupled adenosine receptors are promising therapeutic targets for a wide range of neuropathological conditions, including Parkinson's disease (PD). However, the ubiquity of adenosine receptors and the ultimate lack of selectivity of certain adenosine-based drugs have frequently diminished their therapeutic use. Photopharmacology is a novel approach that allows the spatiotemporal control of receptor function, thus circumventing some of these limitations. Here, we aimed to develop a light-sensitive caged adenosine A_2A receptor (A_2AR) antagonist to photocontrol movement disorders. We synthesized MRS7145 by blocking with coumarin the 5-amino position of the selective A_2AR antagonist SCH442416, which could be photoreleased upon violet light illuminatio

SUBMITTER: Taura J 

PROVIDER: S-EPMC6098950 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature