Discovery of Highly Potent Adenosine A₁ Receptor Agonists: Targeting Positron Emission Tomography Probes.

ABSTRACT: Adenosine receptor (AR) radiotracers for positron emission tomography (PET) have provided knowledge on the in vivo biodistribution of ARs in the central nervous system (CNS), which is of therapeutic interest for various neuropsychiatric disorders. Additionally, radioligands that can image changes in endogenous adenosine levels in different physiological and pathological conditions are still lacking. The binding of known antagonist adenosine A₁ receptor (A₁R) radiotracer, [¹¹C]MDPX, failed to be inhibited by elevated endogenous adenosine in a rodent PET study. Since most of the known AR PET radiotracers were antagonists, we propose that an A₁R agonist radioligand may possess higher sensitivity to measure changes in endogenous adenosine conc

SUBMITTER: Guo M 

PROVIDER: S-EPMC9353746 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature