Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X7 receptor
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2018, Neuroscience and Biobehavioral ReviewsCitation Excerpt :Several CNS-penetrable P2X7 antagonists have been developed by GSK, including GSK compound 16, GSK compound 18, GSK compound 21 and GSK1482160 (Table 1). GSK compound 16, GSK compound 18, and GSK compound 21 inhibit the human P2X7 receptor with IC50 values of 8–10 nM and are much less potent at the rat P2X7 receptor with IC50 values of 80 nM, 398 nM and 63 nM in a dye uptake assay, and B/P ratios of 0.23, 0.33 and <0.1, respectively (Abberley et al., 2010; Beswick et al., 2010). GSK1482160 (GSK compound 31: (Abdi et al., 2010)) exhibits IC50 values of 3 nM and 316 nM at the human and rat P2X7 receptors in a dye uptake assay, respectively, and excellent BBB penetrability with a B/P ratio closing to 2.1 (Abdi et al., 2010).
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