A-839977

A-839977

CAT N°: 30934
Price:

From 48.00 40.80

A-389977 is an antagonist of the purinergic P2X7 receptor.{57152} It inhibits BzATP-evoked intracellular calcium influx in 1321N1 cells expressing human, rat, and mouse receptors (IC50s = 20, 42, and 150 nM, respectively). A-839977 inhibits BzATP-induced YO-PRO dye uptake, a marker of membrane pore formation, and IL-1? release from THP-1 cells (IC50s = 6.6 and 37 nM, respectively). In vivo, A-389977 (30, 100, and 300 µmol/kg, i.p.) reduces thermal hyperalgesia in rats. A-389977 (40 mg/kg) reduces thermal and mechanical hyperalgesia in a rat MRMT-1 mammary carcinoma model of cancer-induced bone pain.{57151}

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