A 438079 hydrochloride
Chemical Name: 3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine hydrochloride
Biological ActivityCompetitive 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
Nelson et al.
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
P2X7-related modulation of pathological nociception in rats.
McGaraughty et al.
Methamphetamine alters microglial immune function through P2X7R signaling.
Fernandes et al.
Citations for A 438079 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for A 438079 hydrochloride include:
45 Citations: Showing 1 - 10
Extracellular ATP Increases Glucose Metabolism in Skeletal Muscle Cells in a P2 Receptor Dependent Manner but Does Not Contribute to Palmitate-Induced Insulin Resistance.
Authors: Miguel Cruz & Beall
Front Physiol 2020;
Amyloid Peptide Induced Neuroinflammation Increases the P2X7 Receptor Expression in Microglial Cells, Impacting on Its Functionality.
Authors: Martínez-Frailes Et al.
Front Cell Neurosci 2019;13:143
ATP-mediated Events in Peritubular Cells Contribute to Sterile Testicular Inflammation.
Authors: Walenta Et al.
Sci Rep 2018;8:1431
Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells.
Authors: Kleiner Et al.
Mol Vis 2018;24:647
Targeting the NLRP3 inflammasome to attenuate spinal cord injury in mice.
J Neuroinflammation 2017;14(1):207
Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP.
Authors: Karmakar Et al.
Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense.
Authors: Ledderose Et al.
J Infect Dis 2016;213:456
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
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
Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via iverm. induces a non-apoptotic and inflammatory form of cancer cell death.
Authors: Draganov Et al.
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
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
Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors.
Authors: Helliwell Et al.
Br J Pharmacol 2015;172:3326
The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
Authors: Giannuzzo Et al.
J Neurosci 2015;14:203
Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells.
Authors: Kowal Et al.
Mol Cancer 2015;13:28
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
The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells.
Authors: Sathanoori Et al.
PLoS One 2015;10:e0125111
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
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
Involvement of the chemokine CCL3 and the purinoceptor P2X7 in the spinal cord in PacT.-induced mechanical allodynia.
Authors: Ochi-Ishi Et al.
Biochem Biophys Res Commun 2014;10:53
Enhanced autophagy blocks angiogenesis via degradation of gastrin-releasing peptide in neuroblastoma cells.
Authors: Kim Et al.
Cell Commun Signal 2013;9:1579
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
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
Natural compounds with P2X7 receptor-modulating properties.
Authors: Fischer Et al.
Purinergic Signal 2013;10:313
ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation.
Authors: Manohar Et al.
J Leukoc Biol 2012;92:787
P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells.
Authors: Gadeock Et al.
Neurosci Lett 2012;8:669
Involvement of connexin43 hemichannel in ATP release after γ-irradiation.
Authors: Ohshima Et al.
Mol Pain 2012;53:551
Regulation of P2X7-dependent inflammatory functions by P2X4 receptor in mouse macrophages.
Authors: Kawano Et al.
Results Immunol 2012;420:102
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
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
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
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
Positive allosteric modulation by iverm. of human but not murine P2X7 receptors.
Authors: Nörenberg Et al.
Br J Pharmacol 2012;167:48
P2X7 receptor activation ameliorates CA3 neuronal damage via a tumor necrosis factor-α-mediated pathway in the rat hippocampus following status epilepticus.
Authors: Kim Et al.
J Neuroinflammation 2011;8:62
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
The P2X7-Egr pathway regulates nucleotide-dependent inflammatory gene expression in microglia.
Authors: Friedle Et al.
Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations.
Authors: Nörenberg Et al.
J Biol Chem 2011;286:11067
Tissue-nonspecific alkaline phosphatase promotes axonal growth of hippocampal neurons.
Authors: Díez-Zaera Et al.
Mol Biol Cell 2011;22:1014
P2X(7) receptor antagonists display agonist-like effects on cell signaling proteins.
Authors: Hedden Et al.
Biochim Biophys Acta 2011;1810:532
The P2X7 receptor-pannexin-1 complex decreases muscarinic acetylcholine receptor-mediated seizure susceptibility in mice.
J Clin Invest 2011;121:2037
Hypertonic stress regulates T cell function via pannexin-1 hemichannels and P2X receptors.
Authors: Woehrle Et al.
J Leukoc Biol 2010;88:1181
P2X7-dependent release of interleukin-1β and nociception in the spinal cord following lipopolysaccharide.
Authors: Clark Et al.
J Radiat Res 2010;30:573
Temporal interleukin-1beta secretion from primary human peripheral blood monocytes by P2X7-independent and P2X7-dependent mechanisms.
Authors: Ward Et al.
J Biol Chem 2010;285:23147
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
Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons.
Authors: Díaz-Hernández Et al.
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