A-839977

P2X7受体拮抗剂；抑制表达人、大鼠和小鼠受体的1321N1细胞中BzATP引起的细胞内钙内流（IC50分别为20、42和150nM）；抑制BzATP诱导的YO-PRO染料摄取和THP-1细胞中IL-1β的释放（IC50分别为6.6和37nM）；以30、100和300µmol/kg腹腔注射剂量降低大鼠的热痛觉过敏；以40mg/kg剂量降低大鼠MRMT-1乳腺癌模型中癌症诱发的骨痛的热痛觉过敏和机械痛觉过敏。A P2X7 receptor antagonist; inhibits BzATP-evoked intracellular calcium influx in 1321N1 cells expressing human, rat, and mouse receptors (IC50s = 20, 42, and 150 nM, respectively); inhibits BzATP-induced YO-PRO dye uptake and IL-1β release from THP-1 cells (IC50s = 6.6 and 37 nM, respectively); reduces thermal hyperalgesia in rats at 30, 100, and 300 µmol/kg, i.p.; reduces thermal and mechanical hyperalgesia in a rat MRMT-1 mammary carcinoma model of cancer-induced bone pain at 40 mg/kg.分子式C19H14Cl2N6O分子量413.3ClC1=CC=CC(N2C(NCC3=CC=CC=C3OC4=CC=CC=N4)=NN=N2)=C1Cl