GSK1370319A is a potent P2X7 antagonist (IC50 = 3.2 nM). GSK1370319A inhibits ATP-induced increase in IL-1beta release and caspase 1 activation in lipopolysaccharide (LPS)-primed mixed glia by blocking assembly of the inflammasome in a pannexin 1-dependent manner. GSK1370319A also inhibits ATP-induced subregion-specific neuronal loss in hippocampal organotypic slice cultures, which is dependent on its ability to prevent inflammasome assembly in glia. Significantly, GSK1370319A attenuates age-related deficits in long-term potentiation (LTP) and inhibits the accompanying age-related caspase 1 activity. We conclude that inhibiting P2X(7) receptor-activated NLRP3 inflammasome formation and the consequent IL-1beta release from glia preserve neuronal viability and synaptic activity.
Molekulargewicht:
301.17
CAS Nummer:
[1001389-31-6]
Formel:
C13H14Cl2N2O2
Target-Kategorie:
Others
T71651
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