Mardepodect 是一种有效的、口服具有活性的、可透过血脑屏障的、选择性的PDE10A抑制剂，IC50=0.37 nM，比作用于其他 PDE 选择性高 1000 多倍。

Mardepodect is a phosphodiesterase inhibitor selective for the PDE10A subtype with an IC50 of 0.37 nM, >1000-fold selectivity over PDE. It is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. Mardepodect can cross the blood-brain barrier.

Mardepodect is active in a range of antipsychotic models with the ED50 of 1 mg/kg, antagonizing apomorphine-induced climbing in mice, inhibiting conditioned avoidance responding in both rats and mice, and blocking N-methyl-D-aspartate antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats, while improving baseline sensory gating in mice.Mardepodect induces a dose-dependent increase in striatal cGMP in mice.

898562-94-2

C25H20N4O

392.45

PF-2545920

DMSO:45 mg/mL (114.66 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years