Description
A CysLT2 receptor antagonist (IC50 = 37.9 nM in a radioligand binding assay); selective for CysLT2 over CysLT1 (IC50 = >30 µM in a radioligand binding assay); inhibits LTD4- or LTC4-induced calcium mobilization in CHO cells expressing human CysLT2 (IC50s = 3.8 and 4.4 nM, respectively); reverses the LTC4-induced increases in perfusion pressure and decreases in contractility in isolated Langendorff-perfused guinea pig hearts; prevents decreases in body weight and neurological deficit scores in a rat model of S. pneumoniae-induced meningitis at 0.1 mg/kg; as well as reduces infarct volume in a rat model of MCAO-induced cerebral ischemia brain injury at 0.1 mg/kg; prevents increases in airway hyperresponsiveness in a mouse model of ovalbumin-induced asthma at 10 mg/kg