Pranlukast (ONO-1078) is a cysteinyl leukotriene receptor-1 antagonist. It antagonizes or reduces bronchospasm caused, principally in asthmatics, by an allergic reaction to accidentally or inadvertently encountered allergens.

LTD4:0.99 nM (Ki), LTC4:5640 nM (Ki), LTE4:0.63 nM (Ki)

Pranlukast在小鼠的缺血性半球的皮质和海马CA1区中明显减少损伤体积,并提高神经元密度.Pranlukast在小鼠的缺血性半球中,还明显地使疤痕壁变薄.

5 mM Pranlukast或Zafirlukast在致敏豚鼠气管中,明显抑制卵清蛋白诱导的分泌分别达70%和65%。Pranlukast或Zafirlukast以浓度依赖的方式明显抑制10 mM LTD4诱发的35SO4输出,10 mM Pranlukast最大的抑制为83%,10 mM 扎鲁司特最大的抑制为78%,IC50值分别为0.3 mM和0.6 mM。Pranlukast在1.3％DMSO-分化的U-937和Jurkat细胞中抑制NF-κB的活化,抑制率分别为40％与30％；和MK-571剂量依赖性抑制NF-κB的活化。Pranlukas和MK-571抑制脂多糖诱导PBMC中的IL-6产生分别约65％和15％。Pranlukast抑制phorbol 12-myristate 13-acetate诱导的NF-κB活化。Pranlukast在NCI-H292细胞中,通过逆转录 - 聚合酶链反应明显抑制脂多糖诱导MUC2 mRNA表达。Pranlukast也抑制HM3-MUC2细胞脂多糖诱导MUC2基因的表达。