Antagonist activity at human CysLT1 receptor expressed in CHO cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
In vivo inhibition of CysLT1 receptor in guinea pig assessed as reduction in LTD4-induced bronchoconstriction at 3 mg/kg, po relative to vehicle treated control
In vivo inhibition of CysLT1 receptor in guinea pig assessed as reduction in LTD4-induced bronchoconstriction at 10 mg/kg, po relative to vehicle treated control
Antagonist activity at human CysLT1 expressed in CHOK1 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
Antiasthmatic activity in guinea pig assessed as inhibition of LTD4-induced bronchoconstriction at 1 mg/kg, po administered 1 hr prior to LTD4 challenge measured over 10 mins relative to control