927691-21-2

PQ-10 is a potent and selective inhibitor of phosphodiesterase type 10 (PDE10; K_i = 4 nM). 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. 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.

PQ-10 is a potent inhibitor of Phosphodiesterase 10A (PDE10A) with IC50 andED50 of 4.6 nM and 13 mg/kg, respectively. PQ-10 induces patterns of brain glucose metabolism which can be a potential translational biomarker. PQ-10 has the potential for researching psychiatric disorders like schizophrenia[1].

PQ-10 is a potent and selective inhibitor of phosphodiesterase 10A (PDE10). Apparently, PQ-10 enhances basic auditory information processing in rats. PQ-10 as other PED10 inhibitors suppresses a growth of human non-small cell lung cancer (NSCLC) cell lines.

PDE10A: 4.6 nM (IC₅₀)

[1] Dedeurwaerdere S, et al. Patterns of brain glucose metabolism induced by phosphodiesterase 10A inhibitors in the mouse: a potential translational biomarker. J Pharmacol Exp Ther. 2011;339(1):210-217. DOI:10.1124/jpet.111.182766