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.
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

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

Showing Results 1 - 10 of 28

  1. Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP.
    Authors: Karmakar Et al.
  2. Active Caspase-1 Induces Plasma Membrane Pores That Precede Pyroptotic Lysis and Are Blocked by Lanthanides
    Authors: Russo Et al.
    The Journal of Immunology
  3. 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.
  4. P2RX7 sensitizes Mac-1/ICAM-1-dependent leukocyte-endothelial adhesion and promotes neurovascular injury during septic encephalopathy.
    Authors: Wang Et al.
    Cell Res
  5. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
    Authors: Giannuzzo Et al.
    J Neurosci
  6. Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells.
    Authors: Kowal Et al.
    Mol Cancer
  7. 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
  8. Extracellular ATP does not induce P2X7 receptor-dependent responses in cultured renal- and liver-derived swine macrophages.
    Authors: Takenouchi Et al.
    Purinergic Signal
  9. 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
  10. Enhanced autophagy blocks angiogenesis via degradation of gastrin-releasing peptide in neuroblastoma cells.
    Authors: Kim Et al.
    Cell Commun Signal
  11. 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
  12. Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes.
    Authors: Foster Et al.
    J Immunol
  13. ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation.
    Authors: Manohar Et al.
    J Leukoc Biol
  14. P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells.
    Authors: Gadeock Et al.
    Neurosci Lett
  15. Involvement of connexin43 hemichannel in ATP release after γ-irradiation.
    Authors: Ohshima Et al.
    Mol Pain
  16. Regulation of P2X7-dependent inflammatory functions by P2X4 receptor in mouse macrophages.
    Authors: Kawano Et al.
    Results Immunol
  17. P2X7 receptor-mediated purinergic signaling promotes liver injury in acetaminophen hepatotoxicity in mice.
    Authors: Hoque Et al.
    Am J Physiol Gastrointest Liver Physiol
  18. ATP induces protein arginine deiminase 2-dependent citrullination in mast cells through the P2X7 purinergic receptor.
    Authors: Arandjelovic Et al.
    J Immunol
  19. Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors.
    Authors: Nörenberg Et al.
    Br J Pharmacol
  20. Purinergic signaling induces cyclooxygenase-1-dependent prostanoid synthesis in microglia: roles in the outcome of excitotoxic brain injury.
    Authors: Anrather Et al.
    PLoS One
  21. The P2X7-Egr pathway regulates nucleotide-dependent inflammatory gene expression in microglia.
    Authors: Friedle Et al.
  22. Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations.
    Authors: Nörenberg Et al.
    J Biol Chem
  23. Tissue-nonspecific alkaline phosphatase promotes axonal growth of hippocampal neurons.
    Authors: Díez-Zaera Et al.
    Mol Biol Cell
  24. P2X(7) receptor antagonists display agonist-like effects on cell signaling proteins.
    Authors: Hedden Et al.
    Biochim Biophys Acta
  25. Hypertonic stress regulates T cell function via pannexin-1 hemichannels and P2X receptors.
    Authors: Woehrle Et al.
    J Leukoc Biol
  26. P2X7-dependent release of interleukin-1β and nociception in the spinal cord following lipopolysaccharide.
    Authors: Clark Et al.
    J Radiat Res
  27. Involvement of SLC17A9-dependent vesicular exocytosis in the mechanism of ATP release during T cell activation.
    Authors: Tokunaga Et al.
    J Biol Chem
  28. Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons.
    Authors: Díaz-Hernández Et al.
Expand to show all
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