Zafirlukast

一种CysLT1受体拮抗剂（在基于细胞的钙动员测定中的IC50=0.014微米）；对CysLT1的选择性高于CysLT2受体（IC50=58微米）；抑制LTD4诱导的孤立豚鼠气管粘液分泌（IC50=0.6微米）；在5微米的浓度下抑制卵清蛋白诱导的卵清蛋白致敏豚鼠气管粘液分泌增加65%；抑制麻醉豚鼠中LTD4诱导的支气管收缩（ED50=61纳摩尔/千克，静脉注射）。A CysLT1 receptor antagonist (IC50 = 0.014 μM in a cell-based calcium mobilization assay); selective for CysLT1 over CysLT2 receptors (IC50 = 58 μM); inhibits LTD4-induced mucus secretion in isolated guinea pig trachea (IC50 = 0.6 μM); inhibits ovalbumin-induced increases in tracheal mucus secretion in ovalbumin-sensitized guinea pigs by 65% at 5 μM; inhibits LTD4-induced bronchoconstriction in anesthetized guinea pigs (ED50 = 61 nmol/kg, i.v.).