Montelukast (sodium salt)

CysLT1受体拮抗剂：一种CysLT1受体拮抗剂（IC50 = 4.9 nM，HEK293细胞膜中表达的人类受体）；对CysLT1受体比CysLT2受体具有更高选择性（IC50 = >10,000 nM）；在麻醉豚鼠模型中，能够抑制LTD4引起的支气管收缩（ED50 = 69 nmol/kg，口服）；在过敏性哮喘小鼠模型中，抑制了椰蛋白引起的气道过敏反应，增加了BALF中的总细胞数和嗜酸性粒细胞数。A CysLT1 receptor antagonist (IC50 = 4.9 nM in HEK293 cell membranes expressing the human receptor); selective for CysLT1 over CysLT2 receptors (IC50 = >10,000 nM in COS-7 cell membranes expressing the human receptor); inhibits LTD4-induced bronchoconstriction in anesthetized guinea pigs (ED50 = 69 nmol/kg, p.o.); inhibits ovalbumin-induced airway hyperresponsiveness and increases in the number of total cells and eosinophils in BALF in a mouse model of allergic asthma at 3 and 10 mg/kg.