Description
A CysLT1 receptor antagonist (Ki = 2.1 nM in a radioligand binding assay using isolated human lung membranes); inhibits contractions induced by LTD4 or LTE4 in histamine-primed isolated guinea pig trachea (pA2 = 9.4 and 9.1, respectively), but not contractions induced by LTC4 in histamine-primed isolated guinea pig trachea at 190 nM; inhibits LTD4-induced calcium mobilization in COS-7 cells expressing the human CysLT1 receptor at 100 nM; improves tissue damping and elasticity, markers of lung function, and decreases IL-4 and IL-5 levels in BALF in a mouse model of ovalbumin-induced asthma at 5 mg/kg