Potent and highly selective A
adenosine antagonist, with a pA
of 9.02 for A
receptors in guinea pig cardiac vasculature and selectivities of 1000, 91 and 500,000 over A
sites respectively. Active
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In vivo characterisation of ZM 241385, a selective adenosine A 2A receptor antagonist.
Keddie et al.
The in vitro pharmacology of ZM 241385, a potent, non-xanthine, A 2a selective adenosine receptor antagonist.
Poucher et al.
Pharmacodynamics of ZM 241385, a potent A 2a adenosine receptor antagonist, after enteric administration in rat, cat and dog.
Poucher et al.
The citations listed below are publications that use Tocris products. Selected citations for ZM 241385 include:
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Anti-inflammatory preconditioning by agonists of adenosine A1 receptor. Authors: Nakav Et al. J Immunol ;3:e2107 Activation of Adenosine 2A receptor inhibits neutrophil apoptosis in an autophagy-dependent manner in mice with systemic inflammatory response syndrome. Authors: Liu Et al. Scientific Reports 2016;6:33614 Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide. Authors: Caiazzo Et al. Biochem.Pharmacol. 2016;112:72 Ticagrelor regulates osteoblast and osteoclast function and promotes bone formation in vivo via an adenosine-dependent mechanism. Authors: Mediero Et al. FASEB J. 2016; Human monocyte recognition of adenosine-based cyclic dinucleotides unveils the A2a Gαs protein-coupled receptor tonic inhibition of mitochondrially induced cell death. Authors: Tosolini Et al. Am J Physiol Lung Cell Mol Physiol 2015;35:479 G-protein coupled receptor solubilization and purification for biophysical analysis and functional studies, in the total absence of detergent. Authors: Jamshad Et al. Mol Cell Biol 2015;35 Deficits in endogenous adenosine formation by ecto-5'-nucleotidase/CD73 impair neuromuscular transmission and immune competence in experimental autoimmune myasthenia gravis. Authors: Oliveira Et al. Mediators Inflamm 2015;2015:460610 Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Authors: Perez-Aso Et al. Arthritis Res Ther 2015;17:249 Application of BRET to monitor ligand binding to GPCRs. Authors: Stoddart Et al. Nat Methods 2015;12:661 Anti-inflammatory effects of adenosine N1-oxide. Authors: Kohno Et al. Biosci Rep 2015;12:2 Creatine, similarly to ketamine, affords antidepressant-like effects in the tail suspension test via adenosine A1 and A2A receptor activation. Authors: Cunha Et al. Biochem J 2015;11:215 Activation of adenosine receptor A2A increases HSC proliferation and inhibits death and senescence by down-regulation of p53 and Rb. Authors: Ahsan and Mehal Front Pharmacol 2014;5:69 IL-6, A1 and A2aR: a crosstalk that modulates BDNF and induces neuroprotection. Authors: Perígolo-Vicente Et al. Biochem Biophys Res Commun 2014;449:477 Cocaine-induced changes of synaptic transmission in the striatum are modulated by adenosine A2A receptors and involve the tyrosine phosphatase STEP. Authors: Chiodi Et al. Neuropsychopharmacology 2014;39:569 Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light. Authors: Ruby Et al. Kidney Int 2014;39:2432 Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation. Authors: Welihinda and Amento Et al. J Inflamm (Lond) 2014;11:37 Cellular signalling pathways mediating dilation of porcine pial arterioles to adenosine A2A receptor activation. Authors: Hein Et al. Blood 2013;99:156 Dopamine D(2) receptor-mediated modulation of adenosine A(2A) receptor agonist binding within the A(2A)R/D(2)R oligomer framework. Authors: Fernández-Dueñas Et al. Oncoimmunology 2013;63:42 Expression of mammalian G protein-coupled receptors in Caenorhabditis elegans. Authors: Jastrzebska Et al. J Neurochem 2013;520:239 Adenosine transporter ENT1 regulates the acquisition of goal-directed behavior and ethanol drinking through A2A receptor in the dorsomedial striatum. Authors: Nam Et al. J Neurosci 2013;33:4329 Adenosine regulates bone metabolism via A1, A2A, and A2B receptors in bone marrow cells from normal humans and patients with multiple myeloma. Authors: He Et al. FASEB J 2013;27:3446 Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth. Authors: Mediavilla-Varela Et al. Neuropsychopharmacology 2013;14:860 When cytokinin, a plant hormone, meets the adenosine A2A receptor: a novel neuroprotectant and lead for treating neurodegenerative disorders? Authors: Lee Et al. PLoS One 2012;7:e38865 A2A adenosine receptor antagonism enhances synaptic and motor effects of cocaine via CB1 cannabinoid receptor activation. Authors: Tozzi Et al. PLoS One 2012;7:e38312 Polyphenol (-)-epigallocatechin gallate-induced cardioprotection may attenuate ischemia-reperfusion injury through adenosine receptor activation: a preliminary study. Authors: Lee Et al. Biomol Ther (Seoul) 2012;63:340 Adenosine A2A receptor activation prevents wear particle-induced osteolysis. Authors: Mediero Et al. Sci Transl Med 2012;4:135ra65 The effect of A(2A) adenosine receptor activation on C-C chemokine receptor 7 expression in human THP1 macrophages during inflammation. Authors: Williams and Cronstein Inflammation 2012;35:614 Autocrine adenosine signaling promotes regulatory T cell-mediated renal protection. Authors: Kinsey Et al. J Am Soc Nephrol 2012;23:1528 Oroxylin A Induces BDNF Expression on Cortical Neurons through Adenosine A2A Receptor Stimulation: A Possible Role in Neuroprotection. Authors: Jeon Et al. Neurochem Int 2012;20:27 CD26 expression and adenosine deaminase activity in regulatory T cells (Treg) and CD4(+) T effector cells in patients with head and neck squamous cell carcinoma. Authors: Mandapathil Et al. FASEB J 2012;1:659 Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay. Authors: Stoddart Et al. Chem Biol 2012;19:1105 CD8+CD45RA+CCR7+FOXP3+ T cells with immunosuppressive properties: a novel subset of inducible human regulatory T cells. Authors: Suzuki Et al. J Immunol 2012;189:2118 Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R. Authors: Fernández-Dueñas Et al. Invest Ophthalmol Vis Sci 2012;123:373 Adenosine A(2A) receptor activation prevents progressive kidney fibrosis in a model of immune-associated chronic inflammation. Authors: Garcia Et al. Proc Natl Acad Sci U S A 2011;80:378 Biophysical mapping of the adenosine A2A receptor. Authors: Zhukov Et al. J Med Chem 2011;54:4312 Cooperation of adenosine with macrophage Toll-4 receptor agonists leads to increased glycolytic flux through the enhanced expression of PFKFB3 gene. Authors: Ruiz-García Et al. J Biol Chem 2011;286:19247 Paeoniflorin suppresses the expression of intercellular adhesion molecule-1 (ICAM-1) in endotoxin-treated human monocytic cells. Authors: Jin Et al. Br J Pharmacol 2011;164:694 A2A adenosine receptor stimulation decreases foam cell formation by enhancing ABCA1-dependent cholesterol efflux. Authors: Bingham Et al. J Leukoc Biol 2010;87:683 Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drug candidate ZM241385. Authors: Wang Et al. Korean J Anesthesiol 2010;5:e13883 The A2aR adenosine receptor controls cytokine production in iNKT cells. Authors: Nowak Et al. Am J Pathol 2010;40:682 Adenosine receptor regulation of coronary blood flow in Ossabaw miniature swine. Authors: Long Et al. J Exp Med 2010;335:781 Adenosine can mediate its actions through generation of reactive oxygen species. Authors: Gebremedhin Et al. J Cereb Blood Flow Metab 2010;30:1777 Generation and accumulation of immunosuppressive adenosine by human CD4+CD25highFOXP3+ regulatory T cells. Authors: Mandapathil Et al. J Biol Chem 2010;285:7176 Adenosine A2A receptor activation protects CD4+ T lymphocytes against activation-induced cell death. Authors: Himer Et al. FASEB J 2010;24:2631 Adenosine A(2A) Receptor Binding Profile of Two Antagonists, ST1535 and KW6002: Consideration on the Presence of Atypical Adenosine A(2A) Binding Sites. Authors: Riccioni Et al. Front Psychiatry 2010;1:22 Activation of A1, A2A, or A3 adenosine receptors attenuates lung ischemia-reperfusion injury. Authors: Gazoni Et al. J Thorac Cardiovasc Surg 2010;140:440 A2A adenosine receptor (AR) activation inhibits pro-inflammatory cytokine production by human CD4+ helper T cells and regulates Helicobacter-induced gastritis and bacterial persistence. Authors: Alam Et al. Mucosal Immunol 2009;2:232 Adenosine-evoked hyperpolarization of retinal ganglion cells is mediated by G-protein-coupled inwardly rectifying K+ and small conductance Ca 2+-activated K+ channel activation. Authors: Clark Et al. J Neurosci 2009;29:11237 Effect of ventilation pressure on alveolar fluid clearance and β-agonist responses in mice. Authors: Yu Et al. Cancer Biol Ther 2009;297:L785 Adenosine A1 and A2a receptors modulate insulinemia, glycemia, and lactatemia in fetal sheep. Authors: Maeda and Koos Proc Natl Acad Sci U S A 2009;296:R693 Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts. Authors: Epperson Et al. Am J Physiol Cell Physiol 2009;296:C1171 A2A adenosine receptor may allow expansion of T cells lacking effector functions in extracellular adenosine-rich microenvironments. Authors: Ohta Et al. Cardiovasc Res 2009;183:5487 The A2B adenosine receptor impairs the maturation and immunogenicity of dendritic cells. Authors: Wilson Et al. J Immunol 2009;182:4616 Large-scale functional expression of WT and truncated human adenosine A2A receptor in Pichia pastoris bioreactor cultures. Authors: Singh Et al. Eur J Immunol 2008;7:28 Mediation of cannabidiol anti-inflammation in the retina by equilibrative nucleoside transporter and A2A adenosine receptor. Authors: Liou Et al. PLoS One 2008;49:5526 Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis. Authors: Garcia Et al. Am J Physiol Regul Integr Comp Physiol 2008;22:445 Adenosine A2A receptor activation inhibits T helper 1 and T helper 2 cell development and effector function. Authors: Csóka Et al. FASEB J 2008;22:3491 Pharmacological blockade of A2A receptors prevents dermal fibrosis in a model of elevated tissue adenosine. Authors: Fernandez Et al. J Pharmacol Exp Ther 2008;172:1675 Synergistic up-regulation of vascular endothelial growth factor (VEGF) expression in macrophages by adenosine A2A receptor agonists and endotoxin involves transcriptional regulation via the hypoxia response element in the VEGF promoter. Authors: Ramanathan Et al. Br J Pharmacol 2007;18:14 Cl-IB-MECA [2-chloro-N6-(3-iodobenzyl)adenosine-5'-N-methylcarboxamide] reduces ischemia/reperfusion injury in mice by activating the A3 adenosine receptor. Authors: Ge Et al. J Inflamm (Lond) 2006;319:1200 Adenosine A2A receptor activation reduces hepatic ischemia reperfusion injury by inhibiting CD1d-dependent NKT cell activation. Authors: Lappas Et al. Mol Biol Cell 2006;203:2639 Adenosine A(2A) receptors play a role in the pathogenesis of hepatic cirrhosis. Authors: Chan Et al. Br J Pharmacol 2006;148:1144 Adenosine A2a receptors induce heterologous desensitization of chemokine receptors. Authors: Zhang Et al. Microb Cell Fact 2006;108:38 Lipopolysaccharide rapidly modifies adenosine receptor transcripts in murine and human macrophages: role of NF-κB in A(2A) adenosine receptor induction. Authors: Murphree Et al. Methods Enzymol 2005;391:575 Calcium increases in retinal glial cells evoked by light-induced neuronal activity. Authors: Newman Blood 2005;25:5502 Pharmacological characterisation of the adenosine receptor mediating increased ion transport in the mouse isolated trachea and the effect of allergen challenge. Authors: Kornerup Et al. Br J Pharmacol 2005;144:1011 A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists. Authors: Jacobson Et al. Chem Biol 2005;12:237 Activation of Th1 and Tc1 cell adenosine A2A receptors directly inhibits IL-2 secretion in vitro and IL-2-driven expansion in vivo. Authors: Erdmann Et al. J Pharmacol Exp Ther 2005;105:4707 Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes. Authors: Germack and Dickenson Br J Pharmacol 2004;141:329 Extracellular ATP and adenosine induce cell apoptosis of human hepatoma Li-7A cells via the A3 adenosine receptor. Authors: Wen and Knowles Br J Pharmacol 2003;140:1009 Neuroprotection by caffeine and adenosine A2A receptor blockade of β-amyloid neurotoxicity. Authors: Dall'Igna Et al. PLoS One 2003;138:1207 Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling. Authors: Nishi Et al. Br J Pharmacol 2003;100:1322 Inhibition of spontaneous acetylcholine secretion by 2-chloroadenosine as revealed by a protein kinase inhibitor at the mouse neuromuscular junction. Authors: Hirsh and Silinsky Br J Pharmacol 2002;135:1897 Adenosine A(2A) receptors in portal hypertension: their role in the abnormal response to adenosine of the cranial mesenteric artery in rabbits. Authors: Brito Et al. J Neurosci 2002;135:1324 Activation of Trk neurotrophin receptors in the absence of neurotrophins. Authors: Lee and Chao Purinergic Signal 2001;98:3555 Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO. Authors: Nieri Et al. Br J Pharmacol 2001;134:745 A(1)-, A(2A)- and A(3)-subtype adenosine receptors modulate intraocular pressure in the mouse. Authors: Avila Et al. Br J Pharmacol 2001;134:241 British Pharmacological Society Meeting. 18-21 December 2000, University of Birmingham. Abstracts. Authors: Slesinger Br J Pharmacol 2001;133 Suppl:1P Dependence of P2-nucleotide receptor agonist-mediated endothelium-independent relaxation on ectonucleotidase activity and A2A-receptors in rat portal vein. Authors: Guibert Et al. Br J Pharmacol 1998;123:1732
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