Inhibition of human recombinant PDE4D3 expressed in baculoviral system using cAMP as substrate at 10 uM by fluorescence polarization assay relative to control
Inhibition of human recombinant PDE4A4 expressed in baculoviral system using cAMP as substrate at 10 uM by fluorescence polarization assay relative to control
Inhibition of human recombinant PDE4B2 expressed in baculoviral system using cAMP as substrate at 10 uM by fluorescence polarization assay relative to control
Inhibition of human recombinant PDE4C2 expressed in baculoviral system using cAMP as substrate at 10 uM by fluorescence polarization assay relative to control
Inhibition of PDE4D in human HTLA-230 cells assessed as increase in forskolin-induced cAMP accumulation at 100 uM pretreated for 10 mins followed by forskolin induction measured after 20 mins by enzyme immunoassay
Toxicity in mouse assessed as sedative effect by measuring reduction of total distance traveled at 10 mg/kg, po measured over 60 mins by open-field test