Pranlukast

口服生物利用度CysLT1受体拮抗剂：一种口服生物利用度的CysLT1受体拮抗剂（IC50 = 4.3-7.2 nM）；对CysLT1受体比CysLT2受体具有更高选择性（对人类受体的IC50 = 3,620 nM）；在分离的豚鼠气管中抑制LTD4诱导的粘液分泌（IC50 = 0.3 µM）；在U937和Jurkat细胞中，抑制TNF-α诱导的NF-ĸB p65核定位（10和100 µM）；抑制豚鼠LTC4、LTD4和LTE4引起的支气管收缩，但对LTB4无效（ID50分别为0.8、1、0.7和>500 µg/kg）；在大鼠MCAO引起的缺血模型中，减少皮层梗死体积81.6%并降低皮层、海马和纹状体的神经元死亡，剂量为0.03 mg/kg。An orally bioavailable CysLT1 receptor antagonist (IC50 = 4.3-7.2 nM); selective for the CysLT1 receptor over the CysLT2 receptor (IC50 = 3,620 nM for the human receptor); inhibits mucus secretion induced by LTD4 in isolated guinea pig trachea (IC50 = 0.3 µM); inhibits TNF-α-induced NF-ĸB p65 nuclear localization in U937 and Jurkat cells at 10 and 100 µM; inhibits bronchoconstriction induced by LTC4, LTD4, and LTE4, but not LTB4, in guinea pigs (ID50s = 0.8, 1, 0.7, and >500 µg/kg, respectively); reduces cortical infarct volume by 81.6% and decreases neuronal death in the cortex, hippocampus, and striatum in a rat model of MCAO-induced ischemia at 0.03 mg/kg.