CGS 21680 hydrochloride
Chemical Name: 4-[2-[[6-Amino-9-(N-ethyl-β-D-ribofuranuronamidosyl)-9H-purin-2-yl]amino]ethyl]benzenepropanoic acid hydrochloride
Biological ActivityA2A 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.
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.
Adenosine receptors and their ligands.
Naunyn Schmiedebergs Arch.Pharmacol., 2000;362:382
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
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 for CGS 21680 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for CGS 21680 hydrochloride include:
72 Citations: Showing 1 - 10
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
PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders.
Authors: Núñez Et al.
Front Pharmacol 2018;9:1200
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
Genome-wide CRISPR Screens in Primary Human T Cells Reveal Key Regulators of Immune Function.
Authors: Shifrut Et al.
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
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
Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide.
Authors: Caiazzo Et al.
Adenosine arrests breast cancer cell motility by A3 receptor stimulation.
Authors: Ledderose Et al.
Purinergic Signalling 2016;
Role of adenosine receptor subtypes in metha. reward and reinforcement.
Authors: Kavanagh Et al.
J Neurogenet 2015;89:265
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
Effects of adenosine A2a receptor agonist and antagonist on cerebellar nuclear factor-kB expression preceded by MDMA toxicity.
Authors: Kermanian Et al.
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
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
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
Presynaptic adenosine A2A receptors dampen cannabinoid CB1 receptor-mediated inhibition of corticostriatal glutamatergic transmission.
Authors: Ferreira Et al.
Br J Pharmacol 2015;172:1074
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
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
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
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
Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light.
Authors: Ruby Et al.
Kidney Int 2014;39:2432
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
Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina.
Authors: Li Et al.
Vis Neurosci 2014;31:237
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
Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation.
Authors: Welihinda and Amento
J Inflamm (Lond) 2014;11:37
Adenosine A2A receptor: a target for regulating renal interstitial fibrosis in obstructive nephropathy.
Authors: Xiao Et al.
PLoS One 2013;8:e60173
Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor.
Authors: Kozma Et al.
Biochem Pharmacol 2013;85:1171
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
Macrophage A2A adenosinergic receptor modulates oxygen-induced augmentation of murine lung injury.
Authors: Aggarwal Et al.
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
Adenosine A2A receptor contributes to ischemic brain damage in newborn piglet.
Authors: Yang Et al.
J Cereb Blood Flow Metab 2013;33:1612
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
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
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
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
Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies.
Authors: Thomas Et al.
Bioorg Med Chem 2013;21:7453
Both MC5r and A2Ar are required for protective regulatory immunity in the spleen of post-experimental autoimmune uveitis in mice.
J Immunol 2013;191:4103
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
Extracellular adenosine signaling induces CX3CL1 expression in the brain to promote experimental autoimmune encephalomyelitis.
Authors: Mills Et al.
J Neurochem 2012;9:193
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
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
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
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.
Adenosine A2A receptor activation prevents wear particle-induced osteolysis.
Authors: Mediero Et al.
Sci Transl Med 2012;4:135ra65
Adenosine A2A receptors in the nucleus accumbens bi-directionally alter cocaine seeking in rats.
Authors: O'Neill Et al.
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
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
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
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
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
Adenosine-induced activation of esophageal nociceptors.
Authors: Ru Et al.
Am J Physiol Gastrointest Liver Physiol 2011;300:G485
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
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
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
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
The A2aR adenosine receptor controls cytokine production in iNKT cells.
Authors: Nowak Et al.
Reinforcing effects of sigma-receptor agonists in rats trained to self-administer cocaine.
Authors: Hiranita Et al.
J Pharmacol Exp Ther 2010;332:515
Adenosine can mediate its actions through generation of reactive oxygen species.
Authors: Gebremedhin Et al.
J Cereb Blood Flow Metab 2010;30:1777
Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors.
Authors: Higley and Sabatini
Nat Neurosci 2010;13:958
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
Adaptation of NS cells growth and differentiation to high-throughput screening-compatible plates.
Authors: Garavaglia Et al.
BMC Neurosci 2010;11:7
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
Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts.
Authors: Epperson Et al.
Am J Physiol Cell Physiol 2009;296:C1171
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
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
Dichotomous DArgic control of striatal synaptic plasticity.
Authors: Shen Et al.
Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis.
Authors: Garcia Et al.
J Neuroinflammation 2008;22:445
Mechanism of adenosine-induced airways obstruction in allergic guinea pigs.
Authors: Keir Et al.
Br J Pharmacol 2006;147:720
The A2B adenosine receptor protects against inflammation and excessive vascular adhesion.
Authors: Yang Et al.
J Clin Invest 2006;116:1913
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
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
Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO.
Authors: Nieri Et al.
Br J Pharmacol 2001;134:745
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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Works perfectly on my CD4 T cells proliferation assay, when detected by CFSE. It inhibited the proliferation of activated CD4 cells in dose-dependent manner.
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