A 438079 hydrochloride

Cat. No. 2972

A 438079 hydrochloride C13H9Cl2N5.HCl [899431-18-6]

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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:
342.61
Formula:
C13H9Cl2N5.HCl
Solubility:
Soluble to 5 mM in water with gentle warming and to 100 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
899431-18-6

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.

Certificate of Analysis / Safety Data Sheet

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Donnelly-Roberts and Jarvis (2007) Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. Br.J.Pharmacol. 151 571. PMID: 17471177.

McGaraughty et al (2007) P2X7-related modulation of pathological nociception in rats. Neuroscience 146 1817. PMID: 17478048.

Nelson et al (2006) Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists. J.Med.Chem. 49 3659. PMID: 16759108.

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Citations are publications that use Tocris products. Selected citations for A 438079 hydrochloride include:

Karmakar et al (2016) Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP. Nat.Commun. 7 10555. PMID: 26877061.

Russo et al (2016) Active Caspase-1 Induces Plasma Membrane Pores That Precede Pyroptotic Lysis and Are Blocked by Lanthanides The Journal of Immunology 197 1353. PMID: 27385779.

Wang et al (2015) P2RX7 sensitizes Mac-1/ICAM-1-dependent leukocyte-endothelial adhesion and promotes neurovascular injury during septic encephalopathy. Cell Res 25 674. PMID: 25998681.

Foster et al (2013) Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes. J Immunol 190 1551. PMID: 23319734.

Ilatovskaya et al (2013) Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli. Am J Physiol Cell Physiol 305 C1050. PMID: 24048730.

Arandjelovic et al (2012) ATP induces protein arginine deiminase 2-dependent citrullination in mast cells through the P2X7 purinergic receptor. J Immunol 189 4112. PMID: 22984079.

Hoque et al (2012) P2X7 receptor-mediated purinergic signaling promotes liver injury in acetaminophen hepatotoxicity in mice. Am J Physiol Gastrointest Liver Physiol 302 G1171. PMID: 22383490.

Manohar et al (2012) ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation. J Leukoc Biol 92 787. PMID: 22753954.

Nörenberg et al (2012) Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors. Br J Pharmacol 167 48. PMID: 22506590.

Anrather et al (2011) Purinergic signaling induces cyclooxygenase-1-dependent prostanoid synthesis in microglia: roles in the outcome of excitotoxic brain injury. PLoS One 6 e25916. PMID: 22022466.

Díez-Zaera et al (2011) Tissue-nonspecific alkaline phosphatase promotes axonal growth of hippocampal neurons. Mol Biol Cell 22 1014. PMID: 21289095.

Friedle et al (2011) The P2X7-Egr pathway regulates nucleotide-dependent inflammatory gene expression in microglia. Glia 59 1. PMID: 20878769.

Hedden et al (2011) P2X(7) receptor antagonists display agonist-like effects on cell signaling proteins. Biochim Biophys Acta 1810 532. PMID: 21397667.

Nörenberg et al (2011) Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations. J Biol Chem 286 11067. PMID: 21262970.

Tokunaga et al (2010) Involvement of SLC17A9-dependent vesicular exocytosis in the mechanism of ATP release during T cell activation. J Biol Chem 285 17406. PMID: 20382737.

Woehrle et al (2010) Hypertonic stress regulates T cell function via pannexin-1 hemichannels and P2X receptors. J Leukoc Biol 88 1181. PMID: 20884646.

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