GSK1482160

GSK1482160 is an antagonist of the purinergic P2X₇ receptor (IC₅₀ = 3.2 nM for the human receptor).¹ It inhibits increases in the levels of reactive oxygen species (ROS) induced by LPS and BzATP (Item No. 15577) in THP-1 macrophages when used at a concentration of 1 µM.² GSK1482160 (20 mg/kg twice per day) decreases the accumulation of misfolded tau aggregates in the brain and improves learning and memory in the Y-maze and contextual fear conditioning tests in human P301S tau transgenic mice.³ It reverses mechanical allodynia in a rat model of chronic constriction injury-induced allodynia when administered at a dose of 20 mg/kg.¹

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1. Abdi, M.H., Beswick, P.J., Billinton, A., et al. Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. Bioorg. Med. Chem. Lett. 20(17), 5080-5084 (2010).

2. Homerin, G., Jawhara, S., Dezitter, X., et al. Pyroglutamide-based P2X7 receptor antagonists targeting inflammatory bowel disease. J. Med. Chem. 63(5), 2074-2094 (2020).

3. Ruan, Z., Delpech, J.-C., Venkatesan Kalavai, S., et al. P2RX7 inhibitor suppresses exosome secretion and disease phenotype in P301S tau transgenic mice. Mol. Neurodegener. 15(1), 47 (2020).