A 839977 is a P2X7 selective antagonist and the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta[1]. 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.

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. A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes[2] and it has been shown to reduce inflammatory and neuropathic pain in animal models[1].

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] and it attenuates dorsal horn neuronal responses in cancer bearing animals[3]. 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].

870061-27-1

C19H14Cl2N6O

413.26

A 839977

DMSO:100 mg/mL (241.98 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years