PF-2545920 (Mardepodect) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM.
PF-2545920 (Mardepodect) displays >1,000-fold selectivity over the PDEs.
PF-2545920 (Mardepodect) antagonizes apomorphine-induced climbing in mice, inhibits conditioned avoidance responding in both rats and mice, and blocks NMDA antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats.
PF-2545920 (Mardepodect) dose-dependently increases c-Fos immunopositive nuclei in all regions of neostriatum in the DRd1a-tdTomato mice.
PF-2545920 (Mardepodect) improves cortico-basal ganglia function in huntington's disease models; orally bioavailable.
