Catalog Number: 1063
Chemical Name: 4-[2-[[6-Amino-9-(N-ethyl-β-D-ribofuranuronamidosyl)-9H-purin-2-yl]amino]ethyl]benzenepropanoic acid hydrochloride
Biological Activity
A2A adenosine receptor agonist (Ki = 27 nM). Has affinity for A1 and A3 adenosine receptors but can be used to distinguish A2A- and A2B-mediated effects.
Technical Data
  • M.Wt:
    535.99
  • Formula:
    C23H29N7O6.HCl
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at -20°C
  • CAS No:
    124431-80-7
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.
Background References
  1. Adenosine receptors and their ligands.
    Klot
    Naunyn Schmiedebergs Arch.Pharmacol., 2000;362:382
  2. Effects of CGS 21680, a selective A2A adenosine receptor agonist, on cardiac output and vascular resistance in acute heart failure in the anaesthetized rat.
    Nekooeian and Tabrizchi
    Br.J.Pharmacol., 1998;123:1666
  3. The selective adenosine A2 receptor agonist, CGS 21680, is a potent depressant of cerebral cortical neuronal activity.
    Phillis et al.
    Brain Res., 1990;509:328
Citations:

The citations listed below are publications that use Tocris products. Selected citations for CGS 21680 hydrochloride include:

55 Citations: Showing 1 - 10
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  1. 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
  2. Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide.
    Authors: Caiazzo Et al.
    Biochem.Pharmacol. 2016;112:72
  3. Adenosine arrests breast cancer cell motility by A3 receptor stimulation.
    Authors: Ledderose Et al.
    Purinergic Signalling 2016;
  4. Role of adenosine receptor subtypes in methamphetamine reward and reinforcement.
    Authors: Kavanagh Et al.
    J Neurogenet 2015;89:265
  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.
    Psychopharmacology (Berl) 2015;35:479
  6. Effects of adenosine A2a receptor agonist and antagonist on cerebellar nuclear factor-kB expression preceded by MDMA toxicity.
    Authors: Kermanian Et al.
    Eneuro 2015;28:120
  7. On the role of A2A and D2 receptors in control of cocaine and food-seeking behaviors in rats.
    Authors: Wydra Et al.
    Am J Respir Cell Mol Biol 2015;232:1767
  8. Selective Effects of PDE10A Inhibitors on Striatopallidal Neurons Require Phosphatase Inhibition by DARPP-32(1,2,3).
    Authors: Polito Et al.
    Mol Cell Biol 2015;2
  9. 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
  10. Adenosine Receptors Differentially Regulate the Expression of Regulators of G-Protein Signalling (RGS) 2, 3 and 4 in Astrocyte-Like Cells.
    Authors: Eusemann Et al.
    PLoS One 2015;10:e0134934
  11. Overexpression of BDNF increases excitability of the lumbar spinal network and leads to robust early locomotor recovery in completely spinalized rats.
    Authors: Ziemlinska Et al.
    PLoS One 2014;9:e88833
  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. Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light.
    Authors: Ruby Et al.
    Kidney Int 2014;39:2432
  15. Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina.
    Authors: Li Et al.
    Vis Neurosci 2014;31:237
  16. Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation.
    Authors: Welihinda and Amento
    J Inflamm (Lond) 2014;11:37
  17. Adenosine A2A receptor: a target for regulating renal interstitial fibrosis in obstructive nephropathy.
    Authors: Xiao Et al.
    PLoS One 2013;8:e60173
  18. Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor.
    Authors: Kozma Et al.
    Biochem Pharmacol 2013;85:1171
  19. 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.
    FASEB J 2013;63:42
  20. Macrophage A2A adenosinergic receptor modulates oxygen-induced augmentation of murine lung injury.
    Authors: Aggarwal Et al.
    Neuropsychopharmacology 2013;48:635
  21. Antagonistic interaction between adenosine A2A receptors and Na+/K+-ATPase-α2 controlling glutamate uptake in astrocytes.
    Authors: Matos Et al.
    J Neurosci 2013;33:18492
  22. Proteasomal degradation of eukaryotic elongation factor-2 kinase (EF2K) is regulated by cAMP-PKA signaling and the SCFβTRCP ubiquitin E3 ligase.
    Authors: Wiseman Et al.
    J Biol Chem 2013;288:17803
  23. 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
  24. Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies.
    Authors: Thomas Et al.
    Bioorg Med Chem 2013;21:7453
  25. Extracellular adenosine signaling induces CX3CL1 expression in the brain to promote experimental autoimmune encephalomyelitis.
    Authors: Mills Et al.
    J Neurochem 2012;9:193
  26. 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
  27. 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
  28. Adenosine A2A receptor activation prevents wear particle-induced osteolysis.
    Authors: Mediero Et al.
    Sci Transl Med 2012;4:135ra65
  29. Adenosine A2A receptors in the nucleus accumbens bi-directionally alter cocaine seeking in rats.
    Authors: O'Neill Et al.
    Neuropsychopharmacology 2012;37:1245
  30. 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
  31. Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R.
    Authors: Fernández-Dueñas Et al.
    J Immunol 2012;123:373
  32. Adenosine A(2A) receptor activation prevents progressive kidney fibrosis in a model of immune-associated chronic inflammation.
    Authors: Garcia Et al.
    PLoS One 2011;80:378
  33. Receptor desensitization and blockade of the suppressive effects of prostaglandin E(2) and adenosine on the cytotoxic activity of human melanoma-infiltrating T lymphocytes.
    Authors: Su Et al.
    Cancer Immunol Immunother 2011;60:111
  34. Adenosine-induced activation of esophageal nociceptors.
    Authors: Ru Et al.
    Am J Physiol Gastrointest Liver Physiol 2011;300:G485
  35. Adenosine A2A receptor activation attenuates tubuloglomerular feedback responses by stimulation of endothelial nitric oxide synthase.
    Authors: Carlström Et al.
    Am J Physiol Renal Physiol 2011;300:F457
  36. Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2A adenosine receptor agonists.
    Authors: Das Et al.
    J Nanobiotechnology 2010;8:11
  37. Multivalent dendrimeric and monomeric adenosine agonists attenuate cell death in HL-1 mouse cardiomyocytes expressing the A(3) receptor.
    Authors: Keene Et al.
    Biochem Pharmacol 2010;80:188
  38. Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drug candidate ZM241385.
    Authors: Wang Et al.
    Biomol Ther (Seoul) 2010;5:e13883
  39. The A2aR adenosine receptor controls cytokine production in iNKT cells.
    Authors: Nowak Et al.
    Neuropharmacology 2010;40:682
  40. Reinforcing effects of sigma-receptor agonists in rats trained to self-administer cocaine.
    Authors: Hiranita Et al.
    J Pharmacol Exp Ther 2010;332:515
  41. Adenosine can mediate its actions through generation of reactive oxygen species.
    Authors: Gebremedhin Et al.
    J Cereb Blood Flow Metab 2010;30:1777
  42. Competitive regulation of synaptic Ca2+ influx by D2 dopamine and A2A adenosine receptors.
    Authors: Higley and Sabatini
    Nat Neurosci 2010;13:958
  43. GSK-3alpha directly regulates beta-adrenergic signaling and the response of the heart to hemodynamic stress in mice.
    Authors: Zhou Et al.
    J Clin Invest 2010;120:2280
  44. Adaptation of NS cells growth and differentiation to high-throughput screening-compatible plates.
    Authors: Garavaglia Et al.
    BMC Neurosci 2010;11:7
  45. 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
  46. Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts.
    Authors: Epperson Et al.
    Am J Physiol Cell Physiol 2009;296:C1171
  47. A2A adenosine receptor may allow expansion of T cells lacking effector functions in extracellular adenosine-rich microenvironments.
    Authors: Ohta Et al.
    Eur J Immunol 2009;183:5487
  48. Dichotomous dopaminergic control of striatal synaptic plasticity.
    Authors: Shen Et al.
    Science 2008;321:848
  49. Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis.
    Authors: Garcia Et al.
    J Neuroinflammation 2008;22:445
  50. Mechanism of adenosine-induced airways obstruction in allergic guinea pigs.
    Authors: Keir Et al.
    Br J Pharmacol 2006;147:720
  51. The A2B adenosine receptor protects against inflammation and excessive vascular adhesion.
    Authors: Yang Et al.
    J Clin Invest 2006;116:1913
  52. 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
  53. 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
  54. Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO.
    Authors: Nieri Et al.
    Br J Pharmacol 2001;134:745
  55. Adenosine A3 receptors on human eosinophils mediate inhibition of degranulation and superoxide anion release.
    Authors: Ezeamuzie and Philips
    Br J Pharmacol 1999;127:188
Expand to show all 55 Citations
Average Rating: 4 (Based on 1 review)

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