Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cell membranes measured after 60 mins by topcount liquid scintillation counting
Antagonist activity at human recombinant M2 receptor expressed in CHO cells assessed as blocking of muscarinic receptor agonist oxotremorine-induced inhibition of forskolin-mediated cAMP accumulation incubated for 10 mins by topcount liquid scintillation counting
Antagonist activity at human recombinant M2 receptor expressed in CHO cell membranes assessed as inhibition of oxotremorine-stimulated [35S]GTPgammaS binding incubated for 60 mins by topcount liquid scintillation counting
Antagonist activity at human recombinant M3 receptor expressed in CHO cells assessed as inhibition of oxotremorine-stimulated intracellular calcium release preincubated for 20 mins followed by oxotremorine addition measured every 0.5 to 1 secs for 15 mins by fluo-4AM dye based FLIPR assay
Bronchoprotective activity in Dunkan-Hartley guinea pig model of acetylcholine-induced bronchoconstriction assessed as efficacious dose that limited bronchrestriction response to 50 ug/mL dose of acetylcholine to doubling of baseline pulmonary resistance administered via nebulization for 10 mins measured at 1.5 hrs post dose by whole body plethysmography
Apparent lung selectivity index, ratio of ID50 for inhibition of pilocarpine-induced salivation in guinea pig administered via nebulization for 10 mins to ID50 for bronchoprotective activity in Dunkan-Hartley guinea pig assessed as inhibition of acetylcholine-induced bronchoconstriction administered via nebulization for 10 mins
Apparent lung selectivity index, ratio of ID50 for inhibition of methacholine-induced depressor response in guinea pig administered via nebulization for 10 mins to ID50 for bronchoprotective activity in Dunkan-Hartley guinea pig assessed as inhibition of acetylcholine-induced bronchoconstriction administered via nebulization for 10 mins
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging