PF-2545920 Mardepodect

PF-2545920, also known as Mardepodect, is a phosphodiesterase inhibitor selective for the PDE10A subtype, which 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. PDE10A inhibitors have shown behavioral effects in rodent models that predict antipsychotic efficacy. PF-2545920 is active in a range of antipsychotic models, 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.

PDE Inhibitors Related Products:

Roflumilast; Sildenafil citrate; Cilomilast; Tadalafil; Pimobendan; GSK256066; Rolipram; Apremilast; Milrinone; Avanafil; Ziritaxestat; Ibudilast; Balipodect; PF8380; Deltarasin; Anagrelide hydrochloride; Enpp-1-IN-1; Crisaborole; CP671305

[1]. Verhoest PR, et al. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. J Med Chem, 2009, 52(16), 5188-5196.

[2]. Grauer SM, et al. Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. J Pharmacol Exp Ther, 2009, 331(2), 574-590.