mardepodect

Mardepodect (PF-2545920) is a phosphodiesterase inhibitor selective for the PDE10A subtype with an IC50 of 0.37 nM and over 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 hydrochloride (Mardepodect HCl) is an orally active, selective and potent inhibitor of PDE10A that crosses the blood-brain barrier (IC50: 0.37 nM).Mardepodect hydrochloride up-regulates the expression of proteins encoding specific growth and transcription factors, cell signalling molecules and cell surface proteins. Mardepodect hydrochloride upregulates genes encoding specific growth factors, transcription factors, cell signalling molecules, and cell surface proteins, while downregulating a broad spectrum of cell cycle and apoptosis-related genes.

[11C]MP 10 (PF-2545920), a specific and effective PDE10A inhibitor (IC50=0.37 nM), is with more than1000-fold specificity activity over the PDE.