SCH 58261

Catalog # Availability Size / Price Qty
SCH 58261 | CAS No. 160098-96-4 | Adenosine A2a Receptor Antagonists
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Description: Potent, highly selective A2A antagonist

Chemical Name: 2-(2-Furanyl)-7-(2-phenylethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine

Purity: ≥99%

Product Details
Citations (42)
Supplemental Products

Biological Activity

SCH 58261 is a potent and selective A2A adenosine receptor competitive antagonist (Ki = 1.3 nM). Displays 323-, 53- and 100-fold selectivity over A1, A2B and A3 receptors, respectively. Reduces melanoma tumor growth and TGF-β levels in WT and P2X7R-null mice.

Technical Data

Soluble 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.

Background References

  1. Binding of the radioligand [3H]-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatal membranes.
    Zocchi et al.
    J.Pharmacol.Exp.Ther., 1996;276:398
  2. Effects of A1 and A2A adenosine receptor ligands in mouse acute models of pain.
    Bastia et al.
    Neurosci.Lett., 2002;328:241
  3. The A2A adenosine receptor mediates coronary vasodilation.
    Belardinelli et al.
    J.Pharmacol.Exp.Ther., 1997;284:1066

Product Datasheets

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Citations for SCH 58261

The citations listed below are publications that use Tocris products. Selected citations for SCH 58261 include:

42 Citations: Showing 1 - 10

  1. Adenosine A2A receptors control synaptic remodeling in the adult brain.
    Authors: Xu Et al.
    Sci Rep  2022;12:14690
  2. A2A receptor contributes to tumor progression in P2X7 null mice.
    Authors: De Marchi Et al.
    Front.Cell Dev.Biol.  2022;10:876510
  3. Functional roles of ST8SIA3-mediated sialylation of striatal DA D2 and adenosine A2A receptors.
    Authors: Lin Et al.
    Transl Psychiatry  2019;9:209
  4. Blockade of microglial adenosine A2A receptor suppresses elevated pressure-induced inflammation, oxidative stress, and cell death in retinal cells.
    Authors: Aires Et al.
    Glia  2019;67:896
  5. Adenosine A2A Receptors in the Rat Prelimbic Medial Prefrontal Cortex Control Delay-Based Cost-Benefit Decision Making.
    Authors: Leffa Et al.
    Front Mol Neurosci  2019;11:475
  6. Anti-Depressant Flu Reveals its Therapeutic Effect Via Astrocytes.
    Authors: Kinoshita Et al.
    EBioMedicine  2018;32:72
  7. Adenosine binds predominantly to adenosine receptor A1 subtype in astrocytes and mediates an immunosuppressive effect.
    Authors: Liu Et al.
    Brain Res  2018;1700:47
  8. Prostaglandin E2-mediated adenosinergic effects on CD14+ cells: Self-amplifying immunosuppression in cancer.
    Authors: Al-Taei Et al.
    Oncoimmunology  2017;6:e1268308
  9. Dominant immunosuppression of dendritic cell function by prostate-cancer-derived exosomes.
    Authors: Salimu Et al.
    J Extracell Vesicles  2017;6:1368823
  10. Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity.
    Authors: Cheng Et al.
    Structure  2017;25:1275
  11. Osteoblastic Lrp4 promotes osteoclastogenesis by regulating ATP release and adenosine-A2AR signaling.
    Authors: Xiong Et al.
    J Cell Biol  2017;216:761
  12. Presynaptic muscarinic acetylcholine autoreceptors (M1, M2 and M4 subtypes), adenosine receptors (A1 and A2A) and tropomyosin-related kinase B receptor (TrkB) modulate the developmental synapse elimination process at the neuromuscular junction.
    Authors: Nadal Et al.
    Cancer Biol Ther  2016;9:67
  13. Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.
    Authors: Zhu Et al.
    Psychopharmacology (Berl)  2015;35:621
  14. Effects of adenosine A2a receptor agonist and antagonist on cerebellar nuclear factor-kB expression preceded by MDMA toxicity.
    Authors: Kermanian Et al.
    J Neuroinflammation  2015;28:120
  15. On the role of A2A and D2 receptors in control of cocaine and food-seeking behaviors in rats.
    Authors: Wydra Et al.
    Mol Brain  2015;232:1767
  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. Adenosine A2AR blockade prevents neuroinflammation-induced death of retinal ganglion cells caused by elevated pressure.
    Authors: Madeira Et al.
    J Neurosci  2015;12:115
  19. Expression and characterization of purinergic receptors in rat middle meningeal artery-potential role in migraine.
    Authors: Haanes and Edvinsson
    Med J Islam Repub Iran  2014;9:e108782
  20. Anti-CD39 and anti-CD73 antibodies A1 and 7G2 improve targeted therapy in ovarian cancer by blocking adenosine-dependent immune evasion.
    Authors: Häusler Et al.
    Neuroscience  2014;6:129
  21. Prolonged adenosine A1 receptor activation in hypoxia and pial vessel disruption focal cortical ischemia facilitates clathrin-mediated AMPA receptor endocytosis and long-lasting synaptic inhibition in rat hippocampal CA3-CA1 synapses: differential regulat
    Authors: Chen Et al.
    J Neurosci  2014;34:9621
  22. Homeostatic control of synaptic activity by endogenous adenosine is mediated by adenosine kinase.
    Authors: Diógenes Et al.
    Cereb Cortex  2014;24:67
  23. Ecto-5'-nucleotidase (CD73)-mediated formation of adenosine is critical for the striatal adenosine A2A receptor functions.
    Authors: Augusto Et al.
    Proc Natl Acad Sci U S A  2013;33:11390
  24. Pannexin 1 channels link chemoattractant receptor signaling to local excitation and global inhibition responses at the front and back of polarized neutrophils.
    Authors: Bao Et al.
    J Biol Chem  2013;288:22650
  25. Opiate-induced changes in brain adenosine levels and narcotic drug responses.
    Authors: Wu Et al.
    J Neuroinflammation  2013;228:235
  26. Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth.
    Authors: Mediavilla-Varela Et al.
    Am J Transl Res  2013;14:860
  27. Pathway-specific modulation of nucleus accumbens in reward and aversive behavior via selective transmitter receptors.
    Authors: Hikida Et al.
    Nat Neurosci  2013;110:342
  28. Extracellular adenosine signaling induces CX3CL1 expression in the brain to promote experimental autoimmune encephalomyelitis.
    Authors: Mills Et al.
    J Neurosci  2012;9:193
  29. Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway.
    Authors: Kan Et al.
    J Virol  2012;86:10338
  30. 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
  31. Adenosine receptor signaling modulates permeability of the blood-brain barrier.
    Authors: Carman Et al.
    J Neurosci  2011;31:13272
  32. Adenosine A2A and A2B receptors are both required for adenosine A1 receptor-mediated cardioprotection.
    Authors: Zhan Et al.
    Am J Physiol Heart Circ Physiol  2011;301:H1183
  33. A(2A) adenosine receptor-mediated increase in coronary flow in hyperlipidemic APOE-knockout mice.
    Authors: Teng and Mustafa
    J Exp Pharmacol  2011;2011:59
  34. Role of aberrant striatal DA D1 receptor/cAMP/protein kinase A/DARPP32 signaling in the paradoxical calming effect of amphetamine.
    Authors: Napolitano Et al.
    J Neurosci  2010;30:11043
  35. Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors.
    Authors: Higley and Sabatini
    Nat Neurosci  2010;13:958
  36. Adaptation of NS cells growth and differentiation to high-throughput screening-compatible plates.
    Authors: Garavaglia Et al.
    BMC Neurosci  2010;11:7
  37. Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts.
    Authors: Xi Et al.
    J Mol Cell Cardiol  2009;47:684
  38. 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
  39. The A2B adenosine receptor impairs the maturation and immunogenicity of dendritic cells.
    Authors: Wilson Et al.
    J Immunol  2009;182:4616
  40. 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
  41. Paraxanthine, the primary metabolite of caffeine, provides protection against DArgic cell death via stimulation of ryanodine receptor channels.
    Authors: Guerreiro Et al.
    Mol Pharmacol  2008;74:980
  42. Dichotomous DArgic control of striatal synaptic plasticity.
    Authors: Shen Et al.
    Science  2008;321:848


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