Cayman Pranlukast

Pranlukast is an orally bioavailable cysteinyl leukotriene 1 (CysLT₁) receptor antagonist (IC₅₀s = 4.3-7.2 nM in radioligand binding assays). It is selective for the CysLT₁ receptor over the CysLT₂ receptor (IC₅₀ = 3,620 nM for the human receptor). Pranlukast inhibits mucus secretion induced by leukotriene D₄ (LTD₄; Item No. ) in isolated guinea pig trachea with an IC₅₀ value of 0.3 µM. It inhibits TNF-α-induced NF-ĸB p65 nuclear localization in U937 and Jurkat cells when used at concentrations of 10 and 100 µM. Pranlukast inhibits bronchoconstriction induced by LTC₄ (Item No. ), LTD₄, and LTE₄ (Item No. ), but not LTB₄ (Item No. ), in guinea pigs (ID₅₀s = 0.8, 1, 0.7, and >500 µg/kg, respectively). 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.

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