Negative allosteric modulation of recombinant human GluN1a/GluN2B expressed in CHO-T-REx cells assessed as inhibition of glutamate/glycine-induced response preincubated for 5 mins followed by glutamate/glycine addition and measured after 5 mins by calcium 5 dye based FLIPR TETRA analysis
Displacement of [3H]-1-(azetidin-1-yl)-2-(6-(4-fluoro-3-methylphenyl)-1H-pyrrolo[3,2-b]pyridin-1-yl)ethanone from rat adult cortex GluN2B receptor measured after 2 hrs by liquid scintillation counting analysis
Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in MDCK-MDR1 cells at 5 uM after 60 mins by LC-MS/MS analysis
Ex vivo receptor occupancy at GluN2B receptor in Sprague-Dawley rat brain assessed as reduction in 3-[3H] 1-(azetidin-1-yl)-2-[6-(4-fluoro-3-methyl-phenyl)pyrrolo[3,2-b]pyridin-1-yl]ethanone receptor labeling at 10 mg/kg, po measured after 0.25 hrs by autoradiography
Ex vivo receptor occupancy at GluN2B receptor in Sprague-Dawley rat brain assessed as reduction in 3-[3H] 1-(azetidin-1-yl)-2-[6-(4-fluoro-3-methyl-phenyl)pyrrolo[3,2-b]pyridin-1-yl]ethanone receptor labeling at 10 mg/kg, po measured after 0.5 hrs by autoradiography
Ex vivo receptor occupancy at GluN2B receptor in Sprague-Dawley rat brain assessed as reduction in 3-[3H] 1-(azetidin-1-yl)-2-[6-(4-fluoro-3-methyl-phenyl)pyrrolo[3,2-b]pyridin-1-yl]ethanone receptor labeling at 10 mg/kg, po measured after 2 hrs by autoradiography