A 438079 hydrochloride

  ( 36 citations )    
Product Datasheet
Catalog Number:2972
Chemical Name:3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine hydrochloride
Product Details
Citations (36)
Supplemental Products
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.
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The citations listed below are publications that use Tocris products. Selected citations for A 438079 hydrochloride include:

36 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. Neuronal Release of Cytokine IL-3 Triggered by Mechanosensitive Autostimulation of the P2X7 Receptor Is Neuroprotective.
    Authors: Lim Et al.
    Front Cell Neurosci  2016;10:270
  5. 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
  6. 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
  7. Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells.
    Authors: Braganhol Et al.
    Biochim Biophys Acta  2015;1852:120
  8. Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors.
    Authors: Helliwell Et al.
    Br J Pharmacol  2015;172:3326
  9. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
    Authors: Giannuzzo Et al.
    J Neurosci  2015;14:203
  10. Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells.
    Authors: Kowal Et al.
    Mol Cancer  2015;13:28
  11. 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
  12. 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
  13. Tanshinone II A sulfonate, but not tanshinone II A, acts as potent negative allosteric modulator of the human purinergic receptor P2X7.
    Authors: Kaiser Et al.
    J Pharmacol Exp Ther  2014;350:531
  14. 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
  15. Enhanced autophagy blocks angiogenesis via degradation of gastrin-releasing peptide in neuroblastoma cells.
    Authors: Kim Et al.
    Cell Commun Signal  2013;9:1579
  16. 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
  17. 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
  18. Natural compounds with P2X7 receptor-modulating properties.
    Authors: Fischer Et al.
    Purinergic Signal  2013;10:313
  19. ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation.
    Authors: Manohar Et al.
    J Leukoc Biol  2012;92:787
  20. P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells.
    Authors: Gadeock Et al.
    Neurosci Lett  2012;8:669
  21. Involvement of connexin43 hemichannel in ATP release after γ-irradiation.
    Authors: Ohshima Et al.
    Mol Pain  2012;53:551
  22. Regulation of P2X7-dependent inflammatory functions by P2X4 receptor in mouse macrophages.
    Authors: Kawano Et al.
    Results Immunol  2012;420:102
  23. 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
  24. P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells.
    Authors: Grol Et al.
    Am J Physiol Endocrinol Metab  2012;302:E561
  25. Mechanisms of ATP release by human trabecular meshwork cells, the enabling step in purinergic regulation of aqueous humor outflow.
    Authors: Li Et al.
    J Cell Physiol  2012;227:172
  26. 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
  27. Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors.
    Authors: Nörenberg Et al.
    Br J Pharmacol  2012;167:48
  28. 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
  29. The P2X7-Egr pathway regulates nucleotide-dependent inflammatory gene expression in microglia.
    Authors: Friedle Et al.
    Glia  2011;59:1
  30. Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations.
    Authors: Nörenberg Et al.
    J Biol Chem  2011;286:11067
  31. Tissue-nonspecific alkaline phosphatase promotes axonal growth of hippocampal neurons.
    Authors: Díez-Zaera Et al.
    Mol Biol Cell  2011;22:1014
  32. P2X(7) receptor antagonists display agonist-like effects on cell signaling proteins.
    Authors: Hedden Et al.
    Biochim Biophys Acta  2011;1810:532
  33. Hypertonic stress regulates T cell function via pannexin-1 hemichannels and P2X receptors.
    Authors: Woehrle Et al.
    J Leukoc Biol  2010;88:1181
  34. P2X7-dependent release of interleukin-1β and nociception in the spinal cord following lipopolysaccharide.
    Authors: Clark Et al.
    J Radiat Res  2010;30:573
  35. 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
  36. 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
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