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:
  • Formula:
  • Solubility:
    Soluble to 5 mM in ethanol and to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
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

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

Showing Results 1 - 10 of 79

  1. Ticagrelor regulates osteoblast and osteoclast function and promotes bone formation in vivo via an adenosine-dependent mechanism.
    Authors: Mediero Et al.
    FASEB J.
  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
  3. Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide.
    Authors: Caiazzo Et al.
  4. 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
  5. 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
  6. 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
  7. Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors.
    Authors: Perez-Aso Et al.
    Arthritis Res Ther
  8. Application of BRET to monitor ligand binding to GPCRs.
    Authors: Stoddart Et al.
    Nat Methods
  9. Anti-inflammatory effects of adenosine N1-oxide.
    Authors: Kohno Et al.
    Biosci Rep
  10. 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
  11. 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
  12. IL-6, A1 and A2aR: a crosstalk that modulates BDNF and induces neuroprotection.
    Authors: Perígolo-Vicente Et al.
    Biochem Biophys Res Commun
  13. 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.
  14. Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light.
    Authors: Ruby Et al.
    Kidney Int
  15. Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation.
    Authors: Welihinda and Amento Et al.
    J Inflamm (Lond)
  16. Cellular signalling pathways mediating dilation of porcine pial arterioles to adenosine A2A receptor activation.
    Authors: Hein Et al.
  17. 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.
  18. Expression of mammalian G protein-coupled receptors in Caenorhabditis elegans.
    Authors: Jastrzebska Et al.
    J Neurochem
  19. 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
  20. 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.
  21. Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth.
    Authors: Mediavilla-Varela Et al.
  22. 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
  23. A2A adenosine receptor antagonism enhances synaptic and motor effects of cocaine via CB1 cannabinoid receptor activation.
    Authors: Tozzi Et al.
    PLoS One
  24. Polyphenol (-)-epigallocatechin gallate-induced cardioprotection may attenuate ischemia-reperfusion injury through adenosine receptor activation: a preliminary study.
    Authors: Lee Et al.
    Biomol Ther (Seoul)
  25. Adenosine A2A receptor activation prevents wear particle-induced osteolysis.
    Authors: Mediero Et al.
    Sci Transl Med
  26. 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
  27. Autocrine adenosine signaling promotes regulatory T cell-mediated renal protection.
    Authors: Kinsey Et al.
    J Am Soc Nephrol
  28. Oroxylin A Induces BDNF Expression on Cortical Neurons through Adenosine A2A Receptor Stimulation: A Possible Role in Neuroprotection.
    Authors: Jeon Et al.
    Neurochem Int
  29. 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.
  30. Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay.
    Authors: Stoddart Et al.
    Chem Biol
  31. CD8+CD45RA+CCR7+FOXP3+ T cells with immunosuppressive properties: a novel subset of inducible human regulatory T cells.
    Authors: Suzuki Et al.
    J Immunol
  32. Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R.
    Authors: Fernández-Dueñas Et al.
    Invest Ophthalmol Vis Sci
  33. 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
  34. Biophysical mapping of the adenosine A2A receptor.
    Authors: Zhukov Et al.
    J Med Chem
  35. 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
  36. Paeoniflorin suppresses the expression of intercellular adhesion molecule-1 (ICAM-1) in endotoxin-treated human monocytic cells.
    Authors: Jin Et al.
    Br J Pharmacol
  37. A2A adenosine receptor stimulation decreases foam cell formation by enhancing ABCA1-dependent cholesterol efflux.
    Authors: Bingham Et al.
    J Leukoc Biol
  38. Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drug candidate ZM241385.
    Authors: Wang Et al.
    Korean J Anesthesiol
  39. The A2aR adenosine receptor controls cytokine production in iNKT cells.
    Authors: Nowak Et al.
    Am J Pathol
  40. Adenosine receptor regulation of coronary blood flow in Ossabaw miniature swine.
    Authors: Long Et al.
    J Exp Med
  41. Adenosine can mediate its actions through generation of reactive oxygen species.
    Authors: Gebremedhin Et al.
    J Cereb Blood Flow Metab
  42. Generation and accumulation of immunosuppressive adenosine by human CD4+CD25highFOXP3+ regulatory T cells.
    Authors: Mandapathil Et al.
    J Biol Chem
  43. Adenosine A2A receptor activation protects CD4+ T lymphocytes against activation-induced cell death.
    Authors: Himer Et al.
  44. 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
  45. Activation of A1, A2A, or A3 adenosine receptors attenuates lung ischemia-reperfusion injury.
    Authors: Gazoni Et al.
    J Thorac Cardiovasc Surg
  46. 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
  47. 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
  48. Effect of ventilation pressure on alveolar fluid clearance and β-agonist responses in mice.
    Authors: Yu Et al.
    Cancer Biol Ther
  49. Adenosine A1 and A2a receptors modulate insulinemia, glycemia, and lactatemia in fetal sheep.
    Authors: Maeda and Koos
    Proc Natl Acad Sci U S A
  50. Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts.
    Authors: Epperson Et al.
    Am J Physiol Cell Physiol
  51. A2A adenosine receptor may allow expansion of T cells lacking effector functions in extracellular adenosine-rich microenvironments.
    Authors: Ohta Et al.
    Cardiovasc Res
  52. The A2B adenosine receptor impairs the maturation and immunogenicity of dendritic cells.
    Authors: Wilson Et al.
    J Immunol
  53. Large-scale functional expression of WT and truncated human adenosine A2A receptor in Pichia pastoris bioreactor cultures.
    Authors: Singh Et al.
    Eur J Immunol
  54. Mediation of cannabidiol anti-inflammation in the retina by equilibrative nucleoside transporter and A2A adenosine receptor.
    Authors: Liou Et al.
    PLoS One
  55. Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis.
    Authors: Garcia Et al.
    Am J Physiol Regul Integr Comp Physiol
  56. Adenosine A2A receptor activation inhibits T helper 1 and T helper 2 cell development and effector function.
    Authors: Csóka Et al.
  57. Pharmacological blockade of A2A receptors prevents dermal fibrosis in a model of elevated tissue adenosine.
    Authors: Fernandez Et al.
    J Pharmacol Exp Ther
  58. 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
  59. 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)
  60. Adenosine A2A receptor activation reduces hepatic ischemia reperfusion injury by inhibiting CD1d-dependent NKT cell activation.
    Authors: Lappas Et al.
    Mol Biol Cell
  61. Adenosine A(2A) receptors play a role in the pathogenesis of hepatic cirrhosis.
    Authors: Chan Et al.
    Br J Pharmacol
  62. Adenosine A2a receptors induce heterologous desensitization of chemokine receptors.
    Authors: Zhang Et al.
    Microb Cell Fact
  63. 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
  64. Calcium increases in retinal glial cells evoked by light-induced neuronal activity.
    Authors: Newman
  65. 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
  66. A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.
    Authors: Jacobson Et al.
    Chem Biol
  67. 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
  68. Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes.
    Authors: Germack and Dickenson
    Br J Pharmacol
  69. 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
  70. Neuroprotection by caffeine and adenosine A2A receptor blockade of β-amyloid neurotoxicity.
    Authors: Dall'Igna Et al.
    PLoS One
  71. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    Br J Pharmacol
  72. 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
  73. 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
  74. Activation of Trk neurotrophin receptors in the absence of neurotrophins.
    Authors: Lee and Chao
    Purinergic Signal
  75. Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO.
    Authors: Nieri Et al.
    Br J Pharmacol
  76. A(1)-, A(2A)- and A(3)-subtype adenosine receptors modulate intraocular pressure in the mouse.
    Authors: Avila Et al.
    Br J Pharmacol
  77. British Pharmacological Society Meeting. 18-21 December 2000, University of Birmingham. Abstracts.
    Authors: Slesinger
    Br J Pharmacol
  78. 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
  79. Anti-inflammatory preconditioning by agonists of adenosine A1 receptor.
    Authors: Nakav Et al.
    J Immunol
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