"目录号: HY-13954
Membrane Transporter/Ion Channel-
A-839977是选择性P2X7受体拮抗剂，能阻断BzATP激发的钙流，对人、大小鼠的P2X7受体的IC50分别为20，42和150 nM。
P2X Receptor
相关产品
A-740003-KN-62-A 438079 (hydrochloride)-ATP disodium salt-AF-353-A-317491-AZD9056 hydrochloride-A-804598-GW791343 dihydrochloride-PSB-12062-Lappaconitine-
生物活性
Description
A-839977 is a novel and selective P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively).IC50 Value: Target: P2X7in vitro: A-839977 potently (IC50=20-150 nM) blocked BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors. A-839977 also potently blocked agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells [1]. in vivo: Systemic administration of A-839977 dose-dependently reduced thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) (ED50=100 micromol/kg, i.p.) in rats. A-839977 also produced robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice (ED50=40 micromol/kg, i.p.), but the antihyperalgesic effects of A-839977 were completely absent in IL-1alphabeta knockout mice [1].
References
[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.