A P2X7 receptor antagonist
A839977 is a novel and selective antagonist of P2X7 receptor with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively [1].
A839977 has been reported to block BzATP-evoked changes in intracellular calcium concentrations in 132N1 cells stable expressing P2X7 receptors with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively. In addition, A839977 has also revealed to inhibit BzATP-stimulated IL-1β release and YO-PRO uptake with the IC50 of 37nM and 7nM, respectively, in differentiated human THP-1 cells. Besides, A839977 has been noted to produce parallel rightward shifts in BzATP concentration-effect calcium influx curves with the pAα value of 8.1. Apart from these, A839977 has been exhibited to reduce CFA-induced thermal hyperalgesia in a dose-dependent fashion with the ED50 value of 100μmol/kg(i.p.) [1].
参考文献:
[1] Honore P1, Donnelly-Roberts D, Namovic M, Zhong C, Wade C, Chandran P, Zhu C, Carroll W, Perez-Medrano A, Iwakura Y, Jarvis MF. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice. Behav Brain Res. 2009 Dec 1;204(1):77-81.
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