PQ-10

PQ-10 is a potent and selective inhibitor of phosphodiesterase type 10 (PDE10; K_i = 4 nM).¹ It has >38-fold selectivity for PDE10 over a panel of 60 CNS-associated receptors, enzymes, and ion channels in vitro. Subcutaneous injection of PQ-10 (32 mg/kg) leads to increases in striatal cGMP and phosphorylation of cAMP response element binding protein (CREB) in murine striatum, known markers of in vivo PDE10 inhibition. PQ-10 at a dose of 0.3 mg/kg, p.o., reduces scopolamine- and MK-801-induced memory deficits in rats.² PQ-10 also inhibits tumor cell growth with IC₅₀ values of 0.29 and 0.22 mM for HCT116 and SW480 colon cancer cells, respectively.³

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1. Chappie, T.A., Humphrey, J.M., Allen, M.P., et al. Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors. J. Med. Chem. 50(2), 182-185 (2007).

2. Reneerkens, O.A.H., Rutten, K., Bollen, E., et al. Inhibition of phoshodiesterase type 2 or type 10 reverses object memory deficits induced by scopolamine or MK-801. Behav. Brain Res. 236(1), 16-22 (2013).

3. Li, N., Lee, K., Zhu, B., et al. Phosphodiesterase 10A: A novel target for selective inhibition of colon tumor cell growth and β-catenin-dependent TCF transcriptional activity. Oncogene 34(12), 1499-1509 (2015).