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).
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