Pranlukast

Pranlukast is an orally bioavailable cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50s = 4.3-7.2 nM in radioligand binding assays).{7174} It is selective for the CysLT1 receptor over the CysLT2 receptor (IC50 = 3,620 nM for the human receptor).{8519} Pranlukast inhibits mucus secretion induced by leukotriene D4 (LTD4; Item No. 20310) in isolated guinea pig trachea with an IC50 value of 0.3 µM.{46532} It inhibits TNF-?-induced NF-?B p65 nuclear localization in U937 and Jurkat cells when used at concentrations of 10 and 100 µM.{46533} Pranlukast inhibits bronchoconstriction induced by LTC4 (Item No. 20210), LTD4, and LTE4 (Item No. 20410), but not LTB4 (Item No. 20110), in guinea pigs (ID50s = 0.8, 1, 0.7, and >500 µg/kg, respectively).{46534} It reduces cortical infarct volume by 81.6% and decreases neuronal death in the cortex, hippocampus, and striatum in a rat model of ischemia induced by middle cerebral artery occlusion (MCAO) when administered at a dose of 0.03 mg/kg.{46535}