CGS 21680 hydrochloride

Catalog # Availability Size / Price Qty
CGS 21680 hydrochloride | CAS No. 124431-80-7 | Adenosine A2a Receptor Agonists
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Description: A2A agonist

Chemical Name: 4-[2-[[6-Amino-9-(N-ethyl-β-D-ribofuranuronamidosyl)-9H-purin-2-yl]amino]ethyl]benzenepropanoic acid hydrochloride

Purity: ≥98%

Product Details
Citations (75)
Supplemental Products
Reviews (1)

Biological Activity

CGS 21680 hydrochloride is a potent A2A adenosine receptor agonist (Ki = 27 nM, EC50 = 1.48-180 nM). CGS 21680 reduces venous resistance, increases heart rate and cardiac output in vivo. In an animal model of Huntington's disease, CGS21680 slows motor deterioration, prevents reduction in brain weight and reduces the size of mutant huntingtin aggregates and intranuclear inclusions. CGS21680 increases proliferation of neural progenitor cells, promotes survival of motoneurons and activates TrkB receptors. Also has anti-inflammatory effects in animal models of lung injury and reduces neurotoxicity induced by Kainate (Cat. No. 7065).

Technical Data

Soluble to 100 mM in DMSO
Desiccate at -20°C

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.

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Citations for CGS 21680 hydrochloride

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

75 Citations: Showing 1 - 10

  1. 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
  2. Adenosine A2A receptors control synaptic remodeling in the adult brain.
    Authors: Xu Et al.
    Sci Rep  2022;12:14690
  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. Adenosine A2a receptor agonist CGS21680 treatment attenuates cardiopulmonary bypass-associated inflammatory lung injury in juvenile rats.
    Authors: Kong Et al.
    Mol.Med.Rep.  2019;20:117
  5. PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders.
    Authors: Núñez Et al.
    Front Pharmacol  2018;9:1200
  6. Melanotan II causes hypothermia in mice by activation of mast cells and stimulation of histamine 1 receptors.
    Authors: Jain Et al.
    Am J Physiol Endocrinol Metab  2018;315:E357
  7. Genome-wide CRISPR Screens in Primary Human T Cells Reveal Key Regulators of Immune Function.
    Authors: Shifrut Et al.
    Cell  2018;175:1958
  8. The Mediating Role of A2A Adenosine Receptors in the Mitochondrial Pathway of Apoptotic Hippocampal Cell Death, Following the Administration of MDMA in Rat.
    Authors: Bakhshayesh Et al.
    Basic Clin Neurosci  2017;8:317
  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. Adenosine arrests breast cancer cell motility by A3 receptor stimulation.
    Authors: Ledderose Et al.
    Purinergic Signalling  2016;
  12. Role of adenosine receptor subtypes in metha. reward and reinforcement.
    Authors: Kavanagh Et al.
    J Neurogenet  2015;89:265
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. Presynaptic adenosine A2A receptors dampen cannabinoid CB1 receptor-mediated inhibition of corticostriatal glutamatergic transmission.
    Authors: Ferreira Et al.
    Br J Pharmacol  2015;172:1074
  19. 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
  20. 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
  21. 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
  22. 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
  23. Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light.
    Authors: Ruby Et al.
    Kidney Int  2014;39:2432
  24. 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
  25. Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina.
    Authors: Li Et al.
    Vis Neurosci  2014;31:237
  26. Persistent reduction of cocaine seeking by pharmacological manipulation of adenosine A1 and A 2A receptors during extinction training in rats.
    Authors: O'Neill Et al.
    Psychopharmacology (Berl)  2014;231:3179
  27. Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation.
    Authors: Welihinda and Amento
    J Inflamm (Lond)  2014;11:37
  28. Adenosine A2A receptor: a target for regulating renal interstitial fibrosis in obstructive nephropathy.
    Authors: Xiao Et al.
    PLoS One  2013;8:e60173
  29. Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor.
    Authors: Kozma Et al.
    Biochem Pharmacol  2013;85:1171
  30. 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.
    FASEB J  2013;63:42
  31. Macrophage A2A adenosinergic receptor modulates oxygen-induced augmentation of murine lung injury.
    Authors: Aggarwal Et al.
    Neuropsychopharmacology  2013;48:635
  32. 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
  33. Adenosine A2A receptor contributes to ischemic brain damage in newborn piglet.
    Authors: Yang Et al.
    J Cereb Blood Flow Metab  2013;33:1612
  34. Intrathecal injection of adenosine 2A receptor agonists reversed neuropathic allodynia through protein kinase (PK)A/PKC signaling.
    Authors: Loram Et al.
    Brain Behav Immun  2013;33:112
  35. 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
  36. 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
  37. 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
  38. Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies.
    Authors: Thomas Et al.
    Bioorg Med Chem  2013;21:7453
  39. Both MC5r and A2Ar are required for protective regulatory immunity in the spleen of post-experimental autoimmune uveitis in mice.
    Authors: Lee
    J Immunol  2013;191:4103
  40. Functional interaction between pre-synaptic α6β2-containing nicotinic and adenosine A2A receptors in the control of DA release in the rat striatum.
    Authors: Garção Et al.
    Br J Pharmacol  2013;169:1600
  41. Extracellular adenosine signaling induces CX3CL1 expression in the brain to promote experimental autoimmune encephalomyelitis.
    Authors: Mills Et al.
    J Neurochem  2012;9:193
  42. 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
  43. Proximal tubule sphingosine kinase-1 has a critical role in A1 adenosine receptor-mediated renal protection from ischemia.
    Authors: Park Et al.
    Kidney Int  2012;82:878
  44. 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
  45. Stimulation of adenosine receptors in the nucleus accumbens reverses the expression of cocaine sensitization and cross-sensitization to DA D2 receptors in rats.
    Authors: Hobson Et al.
    Neuropharmacology  2012;63:1172
  46. Adenosine A2A receptor activation prevents wear particle-induced osteolysis.
    Authors: Mediero Et al.
    Sci Transl Med  2012;4:135ra65
  47. Adenosine A2A receptors in the nucleus accumbens bi-directionally alter cocaine seeking in rats.
    Authors: O'Neill Et al.
    Neuropsychopharmacology  2012;37:1245
  48. 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
  49. 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
  50. 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
  51. 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
  52. 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
  53. Adenosine-induced activation of esophageal nociceptors.
    Authors: Ru Et al.
    Am J Physiol Gastrointest Liver Physiol  2011;300:G485
  54. 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
  55. 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
  56. 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
  57. 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
  58. The A2aR adenosine receptor controls cytokine production in iNKT cells.
    Authors: Nowak Et al.
    Neuropharmacology  2010;40:682
  59. Reinforcing effects of sigma-receptor agonists in rats trained to self-administer cocaine.
    Authors: Hiranita Et al.
    J Pharmacol Exp Ther  2010;332:515
  60. Adenosine can mediate its actions through generation of reactive oxygen species.
    Authors: Gebremedhin Et al.
    J Cereb Blood Flow Metab  2010;30:1777
  61. Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors.
    Authors: Higley and Sabatini
    Nat Neurosci  2010;13:958
  62. 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
  63. Adaptation of NS cells growth and differentiation to high-throughput screening-compatible plates.
    Authors: Garavaglia Et al.
    BMC Neurosci  2010;11:7
  64. 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
  65. Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts.
    Authors: Epperson Et al.
    Am J Physiol Cell Physiol  2009;296:C1171
  66. 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
  67. 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
  68. Dichotomous DArgic control of striatal synaptic plasticity.
    Authors: Shen Et al.
    Science  2008;321:848
  69. Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis.
    Authors: Garcia Et al.
    J Neuroinflammation  2008;22:445
  70. Mechanism of adenosine-induced airways obstruction in allergic guinea pigs.
    Authors: Keir Et al.
    Br J Pharmacol  2006;147:720
  71. The A2B adenosine receptor protects against inflammation and excessive vascular adhesion.
    Authors: Yang Et al.
    J Clin Invest  2006;116:1913
  72. 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
  73. 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
  74. Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO.
    Authors: Nieri Et al.
    Br J Pharmacol  2001;134:745
  75. Adenosine A3 receptors on human eosinophils mediate inhibition of degranulation and superoxide anion release.
    Authors: Ezeamuzie and Philips
    Br J Pharmacol  1999;127:188


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