PW0787 (PW 0787) is a potent, selective, brain-penetrant GPR52 agonist with EC50 of 135 nM in cAMP assays in HEK293 cells.
PW0787displays no significant binding affinity (IC50>10 uM) against other GPCRs, a broad-panel counter screening (NIMH-PDSP), as well as hERG potassium channel.
PW0787 exhibits a good concentration in the brain at 0.25 h with the value of 1807 ng/g and also exhibits an acceptable brain permeability with a brain/plasma ratio of 0.28.
PW0787 is an orally bioavailable and brain-penetrant GPR52 agonist with antipsychotic-like activity, which dose-dependently inhibits amphetamine-evoked hyperactivity in mice.
