Ibudilast

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An inhibitor of PDE4 (IC50s = 54, 65, 239, and 166 nM for PDE4A-D, respectively); selective for PDE4 over PDE1, PDE7A, PDE7B, and PDE9A (IC50 = ≥10,000 nM for all) but does inhibit PDE3A, PDE3B, and PDE5A (IC50s = 1,600, 2,700, and 3,510 nM, respectively); inhibits LPS-induced production of TNF-α and fMLP-induced production of LTB4 in isolated human whole blood (IC50s = 6.2 and 2.5 µM, respectively); inhibits bronchospasm by 34% in a guinea pig model of leukotriene-mediated allergic bronchospasm at 5 mg/kg; prevents increases in TNF-α, IL-1β, and IL-6 expression in the striatum in a mouse model of MPTP-induced Parkinson’s disease; increases striatal expression of GDNF in MPTP-treated and -untreated mice when at 40 and 50 mg/kg, respectively, twice per day