Catalog Number: 2972
Chemical Name: 3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine hydrochloride
Biological Activity
Competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line). Devoid of activity at other P2 receptors (IC50 >> 10 μM). Possesses antinociceptive activity in models of neuropathic pain in vivo. Inhibits methamphetamine-induced microglial migration and phagocytosis in vitro.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 5 mM in water with gentle warming and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
    Nelson et al.
    J.Med.Chem., 2006;49:3659
  2. Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states.
    Donnelly-Roberts and Jarvis
    Br.J.Pharmacol., 2007;151:571
  3. P2X7-related modulation of pathological nociception in rats.
    McGaraughty et al.
    Neuroscience, 2007;146:1817
  4. Methamphetamine alters microglial immune function through P2X7R signaling.
    Fernandes et al.
    J.Neuroinflammation., 2016;13:91

The citations listed below are publications that use Tocris products. Selected citations for A 438079 hydrochloride include:

29 Citations: Showing 1 - 10
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  1. Targeting the NLRP3 inflammasome to attenuate spinal cord injury in mice.
    Authors: Jiang
    J Neuroinflammation 2017;14(1):207
  2. Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP.
    Authors: Karmakar Et al.
    Nat.Commun. 2016;7:10555
  3. Active Caspase-1 Induces Plasma Membrane Pores That Precede Pyroptotic Lysis and Are Blocked by Lanthanides
    Authors: Russo Et al.
    The Journal of Immunology 2016;197:1353
  4. Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via Ivermectin induces a non-apoptotic and inflammatory form of cancer cell death.
    Authors: Draganov Et al.
    Autophagy 2015;5:16222
  5. P2RX7 sensitizes Mac-1/ICAM-1-dependent leukocyte-endothelial adhesion and promotes neurovascular injury during septic encephalopathy.
    Authors: Wang Et al.
    Cell Res 2015;25:674
  6. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
    Authors: Giannuzzo Et al.
    J Neurosci 2015;14:203
  7. Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells.
    Authors: Kowal Et al.
    Mol Cancer 2015;13:28
  8. A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90.
    Authors: Young Et al.
    J Cell Sci 2015;11:113
  9. Extracellular ATP does not induce P2X7 receptor-dependent responses in cultured renal- and liver-derived swine macrophages.
    Authors: Takenouchi Et al.
    Purinergic Signal 2014;4:62
  10. Involvement of the chemokine CCL3 and the purinoceptor P2X7 in the spinal cord in paclitaxel-induced mechanical allodynia.
    Authors: Ochi-Ishi Et al.
    Biochem Biophys Res Commun 2014;10:53
  11. Enhanced autophagy blocks angiogenesis via degradation of gastrin-releasing peptide in neuroblastoma cells.
    Authors: Kim Et al.
    Cell Commun Signal 2013;9:1579
  12. Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli.
    Authors: Ilatovskaya Et al.
    Am J Physiol Cell Physiol 2013;305:C1050
  13. Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes.
    Authors: Foster Et al.
    J Immunol 2013;190:1551
  14. ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation.
    Authors: Manohar Et al.
    J Leukoc Biol 2012;92:787
  15. P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells.
    Authors: Gadeock Et al.
    Neurosci Lett 2012;8:669
  16. Involvement of connexin43 hemichannel in ATP release after γ-irradiation.
    Authors: Ohshima Et al.
    Mol Pain 2012;53:551
  17. Regulation of P2X7-dependent inflammatory functions by P2X4 receptor in mouse macrophages.
    Authors: Kawano Et al.
    Results Immunol 2012;420:102
  18. P2X7 receptor-mediated purinergic signaling promotes liver injury in acetaminophen hepatotoxicity in mice.
    Authors: Hoque Et al.
    Am J Physiol Gastrointest Liver Physiol 2012;302:G1171
  19. ATP induces protein arginine deiminase 2-dependent citrullination in mast cells through the P2X7 purinergic receptor.
    Authors: Arandjelovic Et al.
    J Immunol 2012;189:4112
  20. Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors.
    Authors: Nörenberg Et al.
    Br J Pharmacol 2012;167:48
  21. Purinergic signaling induces cyclooxygenase-1-dependent prostanoid synthesis in microglia: roles in the outcome of excitotoxic brain injury.
    Authors: Anrather Et al.
    PLoS One 2011;6:e25916
  22. The P2X7-Egr pathway regulates nucleotide-dependent inflammatory gene expression in microglia.
    Authors: Friedle Et al.
    Glia 2011;59:1
  23. Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations.
    Authors: Nörenberg Et al.
    J Biol Chem 2011;286:11067
  24. Tissue-nonspecific alkaline phosphatase promotes axonal growth of hippocampal neurons.
    Authors: Díez-Zaera Et al.
    Mol Biol Cell 2011;22:1014
  25. P2X(7) receptor antagonists display agonist-like effects on cell signaling proteins.
    Authors: Hedden Et al.
    Biochim Biophys Acta 2011;1810:532
  26. Hypertonic stress regulates T cell function via pannexin-1 hemichannels and P2X receptors.
    Authors: Woehrle Et al.
    J Leukoc Biol 2010;88:1181
  27. P2X7-dependent release of interleukin-1β and nociception in the spinal cord following lipopolysaccharide.
    Authors: Clark Et al.
    J Radiat Res 2010;30:573
  28. Involvement of SLC17A9-dependent vesicular exocytosis in the mechanism of ATP release during T cell activation.
    Authors: Tokunaga Et al.
    J Biol Chem 2010;285:17406
  29. Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons.
    Authors: Díaz-Hernández Et al.
    Autophagy 2008;121:3717
Expand to show all 29 Citations

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