Description General description A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5 nM against human PDE10A), while exhibiting >500-fold selectivity over other human PDEs 1-11 and little activity against CYP3A4 (IC50 >20 µM) or a panel of 23 kinases (IC50 >30 µM). Reported to be orally available in monkey and rat species and be efficacious in reversing NMDAR antagonist (+)-MK-801- (Cat. No. 475878) induced hyperactivity in a ratsl (MED = 10 mg/kg p.o.) in vivo. A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5 nM against human PDE10A-catalyzed cAMP hydrolysis), while exhibiting >500-fold selectivity over other human PDEs 1-11 and much reduced or little activity against CYP3A4 (IC50 = 7.9 and >20 µM, respectively, with or without preincubation) as well as a panel of 23 kinases (IC50 >30 µM). Reported to be orally available in monkey (AUC0-6 h = 11,496 nM·h, T1/2 = 7.1 h; 3 mg/kg p.o.) and rat (AUC0-6 h475878) induced hyperactivity (1 h post p.o.) in a rat schizophrenia model (MED = 10 mg/kg p.o.) in vivo. Packaging 5 mg in Glass bottle Biochem/physiol Actions Cell permeable: yes Reversible: yes Packaging Packaged under inert gas Warning Toxicity: Standard Handling (A) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Other Notes McElroy, W., et al. 2012. Bioorg. Med. Chem. Lett.22, 1335.