PF-05085727 is a potent inhibitor against cGMP-dependent phosphodiesterase PDE2 (PDE2A; IC50 = 2.3 nM) with >500-fold selectivity over other PDEs. Its 3-[(18)F]fluoroazetidinyl derivative ([(18)F]PF-05270430) has been successfully applied via i.v. injection as a brain-permeant probe for imaging brain PDE2 in live cynomolgus monkeys by positron emission tomography (PET).
Journal of medicinal chemistry, 56(11), 4568-4579 (2013-05-09)
To accelerate the discovery of novel small molecule central nervous system (CNS) positron emission tomography (PET) ligands, we aimed to define a property space that would facilitate ligand design and prioritization, thereby providing a higher probability of success for novel
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