Montelukast

CysLT1受体拮抗剂（在表达人类受体的HEK293细胞膜中IC50=4.9nM）；对CysLT1受体的选择性优于CysLT2受体（在表达人类受体的COS-7细胞膜中IC50=>10,000nM）；抑制麻醉豚鼠LTD4诱发的支气管收缩（ED50=69nmol/kg，口服）；在3和10mg/kg剂量下，抑制卵清蛋白诱发的气道高反应性，并增加过敏性哮喘小鼠模型中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.分子式C35H36ClNO3S分子量586.2CC(C)(O)C(C=CC=C1)=C1CC[C@H](C2=CC(/C=C/C3=NC4=C(C=CC(Cl)=C4)C=C3)=CC=C2)SCC5(CC5)CC(O)=O