Pranlukast

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