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A 438079 hydrochloride
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.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 342.61. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.92 mL||14.59 mL||29.19 mL|
|5 mM||0.58 mL||2.92 mL||5.84 mL|
|10 mM||0.29 mL||1.46 mL||2.92 mL|
|50 mM||0.06 mL||0.29 mL||0.58 mL|
References are publications that support the biological activity of the product.
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
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
Fernandes et al (2016) Methamphetamine alters microglial immune function through P2X7R signaling. J.Neuroinflammation. 13 91 PMID: 27117066
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Keywords: A 438079 hydrochloride, A 438079 hydrochloride supplier, Competitve, P2X7, antagonists, Receptors, Purinergic, purinoceptors, A438079, hydrochloride, P2X, 2972, Tocris Bioscience
44 Citations for A 438079 hydrochloride
Citations are publications that use Tocris products. Selected citations for A 438079 hydrochloride include:
Lim et al (2016) Neuronal Release of Cytokine IL-3 Triggered by Mechanosensitive Autostimulation of the P2X7 Receptor Is Neuroprotective. Front Cell Neurosci 10 270 PMID: 27932954
Woehrle et al (2010) Hypertonic stress regulates T cell function via pannexin-1 hemichannels and P2X receptors. J Leukoc Biol 88 1181 PMID: 20884646
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
Ward et al (2010) Temporal interleukin-1beta secretion from primary human peripheral blood monocytes by P2X7-independent and P2X7-dependent mechanisms. J Biol Chem 285 23147 PMID: 20495003
Braganhol et al (2015) Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells. Biochim Biophys Acta 1852 120 PMID: 25445541
Helliwell et al (2015) Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors. Br J Pharmacol 172 3326 PMID: 25752193
Fischer et al (2013) Natural compounds with P2X7 receptor-modulating properties. Purinergic Signal 10 313 PMID: 24163006
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
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
Nörenberg et al (2012) Positive allosteric modulation by iverm. of human but not murine P2X7 receptors. Br J Pharmacol 167 48 PMID: 22506590
Manohar et al (2012) ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation. J Leukoc Biol 92 787 PMID: 22753954
Martínez-Frailes et al (2019) Amyloid Peptide Induced Neuroinflammation Increases the P2X7 Receptor Expression in Microglial Cells, Impacting on Its Functionality. Front Cell Neurosci 13 143 PMID: 31031598
Jiang (2017) Targeting the NLRP3 inflammasome to attenuate spinal cord injury in mice. J Neuroinflammation 14 207 PMID: 29070054
Sathanoori et al (2015) The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells. PLoS One 10 e0125111 PMID: 25938443
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
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
Li et al (2012) Mechanisms of ATP release by human trabecular meshwork cells, the enabling step in purinergic regulation of aqueous humor outflow. J Cell Physiol 227 172 PMID: 21381023
Grol et al (2012) P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells. Am J Physiol Endocrinol Metab 302 E561 PMID: 22185840
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
Kim et al (2011) P2X7 receptor activation ameliorates CA3 neuronal damage via a tumor necrosis factor-α-mediated pathway in the rat hippocampus following status epilepticus. J Neuroinflammation 8 62 PMID: 21631954
Kim (2011) The P2X7 receptor-pannexin-1 complex decreases muscarinic acetylcholine receptor-mediated seizure susceptibility in mice. J Clin Invest 121 2037 PMID: 21505260
Friedle et al (2011) The P2X7-Egr pathway regulates nucleotide-dependent inflammatory gene expression in microglia. Glia 59 1 PMID: 20878769
Díez-Zaera et al (2011) Tissue-nonspecific alkaline phosphatase promotes axonal growth of hippocampal neurons. Mol Biol Cell 22 1014 PMID: 21289095
Nörenberg et al (2011) Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations. J Biol Chem 286 11067 PMID: 21262970
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
Hedden et al (2011) P2X(7) receptor antagonists display agonist-like effects on cell signaling proteins. Biochim Biophys Acta 1810 532 PMID: 21397667
Ochi-Ishi et al (2014) Involvement of the chemokine CCL3 and the purinoceptor P2X7 in the spinal cord in PacT.-induced mechanical allodynia. Biochem Biophys Res Commun 10 53 PMID: 25127716
Takenouchi et al (2014) Extracellular ATP does not induce P2X7 receptor-dependent responses in cultured renal- and liver-derived swine macrophages. Purinergic Signal 4 62 PMID: 25379376
Kim et al (2013) Enhanced autophagy blocks angiogenesis via degradation of gastrin-releasing peptide in neuroblastoma cells. Cell Commun Signal 9 1579 PMID: 24108003
Díaz-Hernández et al (2008) Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons. Autophagy 121 3717 PMID: 18987356
Walenta et al (2018) ATP-mediated Events in Peritubular Cells Contribute to Sterile Testicular Inflammation. Sci Rep 8 1431 PMID: 29362497
Kleiner et al (2018) Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells. Mol Vis 24 647 PMID: 30310263
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
Draganov et al (2015) Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via iverm. induces a non-apoptotic and inflammatory form of cancer cell death. Autophagy 5 16222 PMID: 26552848
Young et al (2015) A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90. J Cell Sci 11 113 PMID: 25700737
Kowal et al (2015) Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells. Mol Cancer 13 28 PMID: 26050734
Giannuzzo et al (2015) The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells. J Neurosci 14 203 PMID: 26607222
Ledderose et al (2016) Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis 213 456 PMID: 26150546
Kaiser et al (2014) Tanshinone II A sulfonate, but not tanshinone II A, acts as potent negative allosteric modulator of the human purinergic receptor P2X7. J Pharmacol Exp Ther 350 531 PMID: 24970925
Kawano et al (2012) Regulation of P2X7-dependent inflammatory functions by P2X4 receptor in mouse macrophages. Results Immunol 420 102 PMID: 22405772
Ohshima et al (2012) Involvement of connexin43 hemichannel in ATP release after γ-irradiation. Mol Pain 53 551 PMID: 22843620
Gadeock et al (2012) P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells. Neurosci Lett 8 669 PMID: 22661222
Clark et al (2010) P2X7-dependent release of interleukin-1β and nociception in the spinal cord following lipopolysaccharide. J Radiat Res 30 573 PMID: 20071520
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.