ZM 241385

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ZM 241385 | CAS No. 139180-30-6 | Adenosine A2a Receptor Antagonists
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Description: Potent and highly selective A2A antagonist

Chemical Name: 4-(2-[7-Amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol

Purity: ≥99%

Product Details
Citations (109)
Supplemental Products

Biological Activity

ZM 241385 is a potent 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. ZM 241385 suppresses the ERK1/2 pathway in human squamous carcinoma cells.

Technical Data

Soluble to 5 mM in ethanol and to 100 mM in DMSO
Store 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.

Additional Information

Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.

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Citations for ZM 241385

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

109 Citations: Showing 1 - 10

  1. Anti-inflammatory preconditioning by agonists of adenosine A1 receptor.
    Authors: Nakav Et al.
    J Immunol  ;3:e2107
  2. Targeting the Cbl-b-Notch1 axis as a novel immunotherapeutic strategy to boost CD8+ T-cell responses.
    Authors: Monticone Et al.
    Front.Immunol.  2022;13:987298
  3. 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
  4. Number of Circulating CD 73-Expressing Lymphocytes Correlates With Survival After Cardiac Arrest.
    Authors: Ryzhov Et al.
    J Am Heart Assoc  2019;8:e010874
  5. Toll-like receptor 2 induces adenosine receptor A2a and promotes human squamous carcinoma cell growth via extracellular signal regulated kinases �.
    Authors: Palani Et al.
    Oncotarget  2018;9:6814
  6. Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells.
    Authors: Ng
    Cell Signal  2018;51:59
  7. CD150high Bone Marrow Tregs Maintain Hematopoietic Stem Cell Quiescence and Immune Privilege via Adenosine.
    Authors: Hirata Et al.
    Cell Stem Cell  2018;22:445
  8. An Adenosine Receptor for Olfaction in Fish.
    Authors: Wakisaka Et al.
    Curr Biol  2017;27:1437
  9. 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
  10. Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide.
    Authors: Caiazzo Et al.
    Biochem.Pharmacol.  2016;112:72
  11. Ticagrelor regulates osteoblast and osteoclast function and promotes bone formation in vivo via an adenosine-dependent mechanism.
    Authors: Mediero Et al.
    FASEB J.  2016;
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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
  17. Application of BRET to monitor ligand binding to GPCRs.
    Authors: Stoddart Et al.
    Nat Methods  2015;12:661
  18. Anti-inflammatory effects of adenosine N1-oxide.
    Authors: Kohno Et al.
    Biosci Rep  2015;12:2
  19. 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
  20. 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
  21. 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
  22. 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
  23. Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light.
    Authors: Ruby Et al.
    Kidney Int  2014;39:2432
  24. Cardiac myocyte-secreted cAMP exerts paracrine action via adenosine receptor activation.
    Authors: Sassi Et al.
    J Clin Invest  2014;124:5385
  25. Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation.
    Authors: Welihinda and Amento Et al.
    J Inflamm (Lond)  2014;11:37
  26. 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
  27. Cellular signalling pathways mediating dilation of porcine pial arterioles to adenosine A2A receptor activation.
    Authors: Hein Et al.
    Blood  2013;99:156
  28. 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.
    Oncoimmunology  2013;63:42
  29. Expression of mammalian G protein-coupled receptors in Caenorhabditis elegans.
    Authors: Jastrzebska Et al.
    J Neurochem  2013;520:239
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. 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
  36. Enhancement of tumor immunotherapy by deletion of the A2A adenosine receptor.
    Authors: Waickman Et al.
    Cancer Immunol Immunother  2012;61:917
  37. Adenosine A2A receptor activation prevents wear particle-induced osteolysis.
    Authors: Mediero Et al.
    Sci Transl Med  2012;4:135ra65
  38. 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
  39. Autocrine adenosine signaling promotes regulatory T cell-mediated renal protection.
    Authors: Kinsey Et al.
    J Am Soc Nephrol  2012;23:1528
  40. 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
  41. CD73-generated adenosine promotes osteoblast differentiation.
    Authors: Takedachi Et al.
    J Cell Physiol  2012;227:2622
  42. Adenosine receptor activation is responsible for prolonged depression of synaptic transmission after spreading depolarization in brain slices.
    Authors: Lindquist
    Neuroscience  2012;223:365
  43. 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
  44. 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
  45. 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
  46. 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
  47. 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
  48. 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
  49. 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
  50. Biophysical mapping of the adenosine A2A receptor.
    Authors: Zhukov Et al.
    J Med Chem  2011;54:4312
  51. 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
  52. 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
  53. 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
  54. A2A adenosine receptor stimulation decreases foam cell formation by enhancing ABCA1-dependent cholesterol efflux.
    Authors: Bingham Et al.
    J Leukoc Biol  2010;87:683
  55. 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
  56. The A2aR adenosine receptor controls cytokine production in iNKT cells.
    Authors: Nowak Et al.
    Am J Pathol  2010;40:682
  57. Adenosine receptor regulation of coronary blood flow in Ossabaw miniature swine.
    Authors: Long Et al.
    J Exp Med  2010;335:781
  58. Adenosine can mediate its actions through generation of reactive oxygen species.
    Authors: Gebremedhin Et al.
    J Cereb Blood Flow Metab  2010;30:1777
  59. 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
  60. Adenosine A(2) receptors modulate tubuloglomerular feedback.
    Authors: Carlström Et al.
    Am J Physiol Renal Physiol  2010;299:F412
  61. Generation and accumulation of immunosuppressive adenosine by human CD4+CD25highFOXP3+ regulatory T cells.
    Authors: Mandapathil Et al.
    J Biol Chem  2010;285:7176
  62. Adenosine A2A receptor activation protects CD4+ T lymphocytes against activation-induced cell death.
    Authors: Himer Et al.
    FASEB J  2010;24:2631
  63. 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
  64. Activation of A1, A2A, or A3 adenosine receptors attenuates lung ischemia-reperfusion injury.
    Authors: Gazoni Et al.
    J Thorac Cardiovasc Surg  2010;140:440
  65. 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
  66. 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
  67. Effect of ventilation pressure on alveolar fluid clearance and β-agonist responses in mice.
    Authors: Yu Et al.
    Cancer Biol Ther  2009;297:L785
  68. 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
  69. Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts.
    Authors: Epperson Et al.
    Am J Physiol Cell Physiol  2009;296:C1171
  70. 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
  71. The A2B adenosine receptor impairs the maturation and immunogenicity of dendritic cells.
    Authors: Wilson Et al.
    J Immunol  2009;182:4616
  72. 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
  73. 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
  74. 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
  75. 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
  76. Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis.
    Authors: Garcia Et al.
    Am J Physiol Regul Integr Comp Physiol  2008;22:445
  77. 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
  78. 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
  79. 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
  80. 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
  81. 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
  82. 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
  83. Adenosine A(2A) receptors play a role in the pathogenesis of hepatic cirrhosis.
    Authors: Chan Et al.
    Br J Pharmacol  2006;148:1144
  84. Adenosine A2a receptors induce heterologous desensitization of chemokine receptors.
    Authors: Zhang Et al.
    Microb Cell Fact  2006;108:38
  85. 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
  86. Calcium increases in retinal glial cells evoked by light-induced neuronal activity.
    Authors: Newman
    Blood  2005;25:5502
  87. 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
  88. 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
  89. 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
  90. 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
  91. Role of adenosine A2A receptor in the regulation of gastric somatostatin release.
    Authors: Yip
    J Pharmacol Exp Ther  2004;309:804
  92. 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
  93. 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
  94. Neuroprotection by caffeine and adenosine A2A receptor blockade of β-amyloid neurotoxicity.
    Authors: Dall'Igna Et al.
    PLoS One  2003;138:1207
  95. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    Br J Pharmacol  2003;100:1322
  96. 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
  97. 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
  98. 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
  99. Activation of Trk neurotrophin receptors in the absence of neurotrophins.
    Authors: Lee and Chao
    Purinergic Signal  2001;98:3555
  100. Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO.
    Authors: Nieri Et al.
    Br J Pharmacol  2001;134:745
  101. 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
  102. British Pharmacological Society Meeting. 18-21 December 2000, University of Birmingham. Abstracts.
    Authors: Slesinger
    Br J Pharmacol  2001;133 Suppl:1P
  103. 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
  104. A(2A) adenosine receptor mediated potassium channel activation in rat epididymal smooth muscle.
    Authors: Haynes
    Br J Pharmacol  2000;130:685
  105. 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
  106. 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
  107. 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
  108. 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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