产品描述:
HAMI3379 is a cysteinyl leukotriene 2 (CysLT2) receptor antagonist (IC50 = 37.9 nM in a radioligand binding assay).{18145} It is selective for CysLT2 over CysLT1 (IC50 = >30 µM in a radioligand binding assay). HAMI3379 inhibits calcium mobilization induced by leukotriene D4 (LTD4; Item No. 20310) or leukotriene C4 (LTC4; Item No. 20210) in CHO cells expressing human CysLT2 (IC50s = 3.8 and 4.4 nM, respectively). It reverses the LTC4-induced increases in perfusion pressure and decreases in contractility in isolated Langendorff-perfused guinea pig hearts in a concentration-dependent manner. HAMI3379 (0.1 mg/kg) prevents decreases in body weight and neurological deficit scores in a rat model of S. pneumoniae-induced meningitis, as well as reduces infarct volume in a rat model of cerebral ischemia brain injury induced by middle cerebral artery occlusion (MCAO).{62970,62971} It also prevents increases in airway hyperresponsiveness in a mouse model of ovalbumin-induced asthma when administered at a dose of 10 mg/kg.{62972}