Chemical Name: 4-(2-[7-Amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol
Biological ActivityPotent and highly selective A2A adenosine antagonist, with a pA2 of 9.02 for A2A receptors in guinea pig cardiac vasculature and fold selectivities of 1000, 91 and 500,000 over A1, A2B and A3 sites respectively. Active in vivo.
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.
In vivo characterisation of ZM 241385, a selective adenosine A2A receptor antagonist.
Keddie et al.
The in vitro pharmacology of ZM 241385, a potent, non-xanthine, A2a selective adenosine receptor antagonist.
Poucher et al.
Pharmacodynamics of ZM 241385, a potent A2a adenosine receptor antagonist, after enteric administration in rat, cat and dog.
Poucher et al.
Citations for ZM 241385
The citations listed below are publications that use Tocris products. Selected citations for ZM 241385 include:
106 Citations: Showing 1 - 10
Anti-inflammatory preconditioning by agonists of adenosine A1 receptor.
Authors: Nakav Et al.
J Immunol ;3:e2107
Adenosine A2A receptor stimulation restores cell functions and differentiation in Niemann-Pick type C-like oligodendrocytes.
Authors: Nuccio Et al.
Sci Rep 2019;9:9782
Number of Circulating CD 73-Expressing Lymphocytes Correlates With Survival After Cardiac Arrest.
Authors: Ryzhov Et al.
J Am Heart Assoc 2019;8:e010874
Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells.
Cell Signal 2018;51:59
CD150high Bone Marrow Tregs Maintain Hematopoietic Stem Cell Quiescence and Immune Privilege via Adenosine.
Authors: Hirata Et al.
Cell Stem Cell 2018;22:445
An Adenosine Receptor for Olfaction in Fish.
Authors: Wakisaka Et al.
Curr Biol 2017;27:1437
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.
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
Critical Role of Mast Cells and Peroxisome Proliferator-Activated Receptor γ in the Induction of Myeloid-Derived Suppressor Cells by Marijuana Cannabidiol In Vivo.
Authors: Hegde Et al.
J Immunol 2015;194:5211
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 KA, 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.
Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light.
Authors: Ruby Et al.
Kidney Int 2014;39:2432
Cardiac myocyte-secreted cAMP exerts paracrine action via adenosine receptor activation.
Authors: Sassi Et al.
J Clin Invest 2014;124:5385
Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation.
Authors: Welihinda and Amento Et al.
J Inflamm (Lond) 2014;11:37
Regulatory T cells negatively affect IL-2 production of effector T cells through CD39/adenosine pathway in HIV infection.
Authors: Jenabian Et al.
PLoS Pathog 2013;9:e1003319
Cellular signalling pathways mediating dilation of porcine pial arterioles to adenosine A2A receptor activation.
Authors: Hein Et al.
DA 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.
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.
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
Enhancement of tumor immunotherapy by deletion of the A2A adenosine receptor.
Authors: Waickman Et al.
Cancer Immunol Immunother 2012;61:917
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
Autocrine adenosine signaling promotes regulatory T cell-mediated renal protection.
Authors: Kinsey Et al.
J Am Soc Nephrol 2012;23:1528
The effect of adenosine A(2A) receptor antagonists on hydroxyl radical, DA, and glutamate in the striatum of rats with altered function of VMAT2.
Authors: Golembiowska and Dziubina
Neurotox Res 2012;22:150
CD73-generated adenosine promotes osteoblast differentiation.
Authors: Takedachi Et al.
J Cell Physiol 2012;227:2622
Adenosine receptor activation is responsible for prolonged depression of synaptic transmission after spreading depolarization in brain slices.
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
Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency virus-1 Tat-mediated activation of microglial cells.
Authors: Kiebala and Maggirwar
PLoS One 2011;6:e18633
Biophysical mapping of the adenosine A2A receptor.
Authors: Zhukov Et al.
J Med Chem 2011;54:4312
The distinct role of medium spiny neurons and cholinergic interneurons in the D2/A2A receptor interaction in the striatum: implications for Parkinson's disease.
Authors: Tozzi Et al.
J Neurosci 2011;31:1850
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
Interactions between adenosine and K+ channel-related pathways in the coupling of somatosensory activation and pial arteriolar dilation.
Authors: Paisansathan Et al.
Am J Physiol Heart Circ Physiol 2010;299:H2009
Adenosine A(2) receptors modulate tubuloglomerular feedback.
Authors: Carlström Et al.
Am J Physiol Renal Physiol 2010;299:F412
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 Ca2+-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 Insemia, 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
The adenosine A2A receptor antagonist ZM241385 enhances neuronal survival after oxygen-glucose deprivation in rat CA1 hippocampal slices.
Authors: Pugliese Et al.
Br J Pharmacol 2009;157:818
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
Interaction of mechanisms involving epoxyeicosatrienoic acids, adenosine receptors, and metabotropic glutamate receptors in neurovascular coupling in rat whisker barrel cortex.
Authors: Shi Et al.
J Cereb Blood Flow Metab 2008;28:111
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
Characterization of human and rodent native and recombinant adenosine A(2B) receptors by radioligand binding studies.
Authors: Bertarelli Et al.
Purinergic Signal 2006;2:559
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.
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
Facilitation of noradrenaline release by activation of adenosine A(2A) receptors triggers both phospholipase C and adenylate cyclase pathways in rat tail artery.
Authors: Fresco Et al.
Cardiovasc Res 2004;63:739
Role of adenosine A2A receptor in the regulation of gastric somatostatin release.
J Pharmacol Exp Ther 2004;309:804
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
2-Chloroadenosine but not adenosine induces apoptosis in rheumatoid fibroblasts independently of cell surface adenosine receptor signalling.
Authors: Koshiba Et al.
Br J Pharmacol 2002;135:1477
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.
Br J Pharmacol 2001;133 Suppl:1P
Accelerated resequestration of cytosolic calcium and suppression of the pro-inflammatory activities of human neutrophils by CGS 21680 in vitro.
Authors: Anderson Et al.
Br J Pharmacol 2000;130:717
A(2A) adenosine receptor mediated potassium channel activation in rat epididymal smooth muscle.
Br J Pharmacol 2000;130:685
Effect of A2A adenosine receptor stimulation and antagonism on synaptic depression induced by in vitro ischaemia in rat hippocampal slices.
Authors: Latini Et al.
Br J Pharmacol 1999;128:1035
A2B adenosine receptors mediate relaxation of the pig intravesical ureter: adenosine modulation of non adrenergic non cholinergic excitatory neurotransmission.
Authors: Hernandez Et al.
Br J Pharmacol 1999;126:969
A1 and A2 adenosine receptor modulation of contractility in the cauda epididymis of the guinea-pig.
Authors: Haynes Et al.
Br J Pharmacol 1998;125:570
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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