| Bioactivity | A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta[1]. | ||||||||||||
| Target | IC50: of 20 nM (human P2X7 receptor), 42 nM (rat P2X7 receptor), 150 nM (mouse P2X7 receptor) | ||||||||||||
| Invitro | A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors, (IC50=20-150 nM), which blocks agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells, it has been shown to reduce inflammatory and neuropathic pain in animal models[1].A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes[2]. RT-PCR[2] Cell Line: | ||||||||||||
| In Vivo | A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats[1].A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice[1].A 839977 attenuates dorsal horn neuronal responses in cancer bearing animals[3]. Animal Model: | ||||||||||||
| Name | A 839977 | ||||||||||||
| CAS | 870061-27-1 | ||||||||||||
| Formula | C19H14Cl2N6O | ||||||||||||
| Molar Mass | 413.26 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Honore P, et al. 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. [2]. Albalawi F et.al, The P2X7 Receptor Primes IL-1β and the NLRP3 Inflammasome in Astrocytes Exposed to Mechanical Strain. Front Cell Neurosci. 2017 Aug 8;11:227 [3]. Falk S et al.P2X7 receptor-mediated analgesia in cancer-induced bone pain. Neuroscience. 2015 Apr 16; 291:93-105. |
A 839977
CAS: 870061-27-1 F: C19H14Cl2N6O W: 413.26
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7
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