Chemical Name: 1-(2,3-Dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine
Biological ActivityA 839977 is a potent P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively). Displays antinociceptive effects in rat and mice models of inflammatory pain. CNS penetrant.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1αβ knockout mice.
Honore et al.
Recent patents on novel P2X7 receptor antagonists and their potential for reducing central nervous system inflammation.
Friedle et al.
Recent Pat.CNS Drug Discov., 2010;5:35
Citation for A 839977
The citations listed below are publications that use Tocris products. Selected citations for A 839977 include:
1 Citation: Showing 1 - 1
Caveolin-1 regulates P2X7 receptor signaling in osteoblasts.
Authors: Gangadharan Et al.
PLoS One 2015;308:C41
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