Catalog Number: 1036
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 Activity
Potent and highly selective A2A adenosine antagonist, with a pA2 of 9.02 for A2A receptors in guinea pig cardiac vasculature and selectivities of 1000, 91 and 500,000 over A1, A2B and A3 sites respectively. Active in vivo.
Technical Data
  • M.Wt:
    337.34
  • Formula:
    C16H15N7O2
  • Solubility:
    Soluble to 5 mM in ethanol and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    139180-30-6
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.
Additional Information
Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.
Background References
  1. In vivo characterisation of ZM 241385, a selective adenosine A2A receptor antagonist.
    Keddie et al.
    Eur.J.Pharmacol., 1996;301:107
  2. The in vitro pharmacology of ZM 241385, a potent, non-xanthine, A2a selective adenosine receptor antagonist.
    Poucher et al.
    Br.J.Pharmacol., 1995;115:1096
  3. Pharmacodynamics of ZM 241385, a potent A2a adenosine receptor antagonist, after enteric administration in rat, cat and dog.
    Poucher et al.
    J.Pharm.Pharmacol., 1996;48:601
Citations:

The citations listed below are publications that use Tocris products. Selected citations for ZM 241385 include:

79 Citations: Showing 1 - 10
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  1. Anti-inflammatory preconditioning by agonists of adenosine A1 receptor.
    Authors: Nakav Et al.
    J Immunol ;3:e2107
  2. 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
  3. Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide.
    Authors: Caiazzo Et al.
    Biochem.Pharmacol. 2016;112:72
  4. Ticagrelor regulates osteoblast and osteoclast function and promotes bone formation in vivo via an adenosine-dependent mechanism.
    Authors: Mediero Et al.
    FASEB J. 2016;
  5. 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
  6. 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
  7. 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
  8. 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
  9. Application of BRET to monitor ligand binding to GPCRs.
    Authors: Stoddart Et al.
    Nat Methods 2015;12:661
  10. Anti-inflammatory effects of adenosine N1-oxide.
    Authors: Kohno Et al.
    Biosci Rep 2015;12:2
  11. 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
  12. 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
  13. 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
  14. 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
  15. Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light.
    Authors: Ruby Et al.
    Kidney Int 2014;39:2432
  16. Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation.
    Authors: Welihinda and Amento Et al.
    J Inflamm (Lond) 2014;11:37
  17. Cellular signalling pathways mediating dilation of porcine pial arterioles to adenosine A2A receptor activation.
    Authors: Hein Et al.
    Blood 2013;99:156
  18. 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
  19. Expression of mammalian G protein-coupled receptors in Caenorhabditis elegans.
    Authors: Jastrzebska Et al.
    J Neurochem 2013;520:239
  20. 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
  21. 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
  22. 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
  23. 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
  24. 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
  25. 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
  26. Adenosine A2A receptor activation prevents wear particle-induced osteolysis.
    Authors: Mediero Et al.
    Sci Transl Med 2012;4:135ra65
  27. 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
  28. Autocrine adenosine signaling promotes regulatory T cell-mediated renal protection.
    Authors: Kinsey Et al.
    J Am Soc Nephrol 2012;23:1528
  29. 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
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. Biophysical mapping of the adenosine A2A receptor.
    Authors: Zhukov Et al.
    J Med Chem 2011;54:4312
  36. 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
  37. 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
  38. A2A adenosine receptor stimulation decreases foam cell formation by enhancing ABCA1-dependent cholesterol efflux.
    Authors: Bingham Et al.
    J Leukoc Biol 2010;87:683
  39. 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
  40. The A2aR adenosine receptor controls cytokine production in iNKT cells.
    Authors: Nowak Et al.
    Am J Pathol 2010;40:682
  41. Adenosine receptor regulation of coronary blood flow in Ossabaw miniature swine.
    Authors: Long Et al.
    J Exp Med 2010;335:781
  42. Adenosine can mediate its actions through generation of reactive oxygen species.
    Authors: Gebremedhin Et al.
    J Cereb Blood Flow Metab 2010;30:1777
  43. Generation and accumulation of immunosuppressive adenosine by human CD4+CD25highFOXP3+ regulatory T cells.
    Authors: Mandapathil Et al.
    J Biol Chem 2010;285:7176
  44. Adenosine A2A receptor activation protects CD4+ T lymphocytes against activation-induced cell death.
    Authors: Himer Et al.
    FASEB J 2010;24:2631
  45. 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
  46. Activation of A1, A2A, or A3 adenosine receptors attenuates lung ischemia-reperfusion injury.
    Authors: Gazoni Et al.
    J Thorac Cardiovasc Surg 2010;140:440
  47. 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
  48. 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
  49. Effect of ventilation pressure on alveolar fluid clearance and β-agonist responses in mice.
    Authors: Yu Et al.
    Cancer Biol Ther 2009;297:L785
  50. 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
  51. Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts.
    Authors: Epperson Et al.
    Am J Physiol Cell Physiol 2009;296:C1171
  52. 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
  53. The A2B adenosine receptor impairs the maturation and immunogenicity of dendritic cells.
    Authors: Wilson Et al.
    J Immunol 2009;182:4616
  54. 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
  55. 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
  56. Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis.
    Authors: Garcia Et al.
    Am J Physiol Regul Integr Comp Physiol 2008;22:445
  57. 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
  58. 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
  59. 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
  60. 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
  61. 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
  62. Adenosine A(2A) receptors play a role in the pathogenesis of hepatic cirrhosis.
    Authors: Chan Et al.
    Br J Pharmacol 2006;148:1144
  63. Adenosine A2a receptors induce heterologous desensitization of chemokine receptors.
    Authors: Zhang Et al.
    Microb Cell Fact 2006;108:38
  64. 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
  65. Calcium increases in retinal glial cells evoked by light-induced neuronal activity.
    Authors: Newman
    Blood 2005;25:5502
  66. 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
  67. 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
  68. 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
  69. 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
  70. 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
  71. Neuroprotection by caffeine and adenosine A2A receptor blockade of β-amyloid neurotoxicity.
    Authors: Dall'Igna Et al.
    PLoS One 2003;138:1207
  72. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    Br J Pharmacol 2003;100:1322
  73. 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
  74. 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
  75. Activation of Trk neurotrophin receptors in the absence of neurotrophins.
    Authors: Lee and Chao
    Purinergic Signal 2001;98:3555
  76. Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO.
    Authors: Nieri Et al.
    Br J Pharmacol 2001;134:745
  77. 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
  78. British Pharmacological Society Meeting. 18-21 December 2000, University of Birmingham. Abstracts.
    Authors: Slesinger
    Br J Pharmacol 2001;133 Suppl:1P
  79. 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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