CGS 21680 hydrochloride

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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% (HPLC)
Citations (75)
Reviews (2)
Literature (1)

Biological Activity for CGS 21680 hydrochloride

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).

Compound Libraries for CGS 21680 hydrochloride

CGS 21680 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for CGS 21680 hydrochloride

M. Wt 535.99
Formula C23H29N7O6.HCl
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 124431-80-7
PubChem ID 10256643
Smiles NC1=NC(NCCC4=CC=C(CCC(O)=O)C=C4)=NC2=C1N=CN2[C@@H]3O[C@H]([C@](NCC)=O)[C@@H](O)[C@H]3O.Cl

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.

Solubility Data for CGS 21680 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 53.6 100

Preparing Stock Solutions for CGS 21680 hydrochloride

The following data is based on the product molecular weight 535.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.87 mL 9.33 mL 18.66 mL
5 mM 0.37 mL 1.87 mL 3.73 mL
10 mM 0.19 mL 0.93 mL 1.87 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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Product Datasheets for CGS 21680 hydrochloride

Certificate of Analysis / Product Datasheet
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References for CGS 21680 hydrochloride

References are publications that support the biological activity of the product.

Klot (2000) Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch.Pharmacol. 362 382 PMID: 11111832

Nekooeian and Tabrizchi (1998) Effects of CGS 21680, a selective A2A adenosine receptor agonist, on cardiac output and vascular resistance in acute heart failure in the anaesthetized rat. Br.J.Pharmacol. 123 1666 PMID: 9605574

Phillis et al (1990) The selective adenosine A2 receptor agonist, CGS 21680, is a potent depressant of cerebral cortical neuronal activity. Brain Res. 509 328 PMID: 2322828

Chou et al (2005) CGS21680 attenuates symptoms of Huntington's disease in a transgenic mouse model. J.Neurochem. 93 310 PMID: 15816854

Wiese et al (2007) Adenosine receptor A2A-R contributes to motoneuron survival by transactivating the tyrosine kinase receptor TrkB Proc.Natl.Acad.Sci.U.S.A. 104 17210 PMID: 17940030

Rebola et al (2005) Different roles of adenosine A1, A2A and A3 receptors in controlling kainate-induced toxicity in cortical cultured neurons. Neurochem.Int. 47 317 PMID: 16011860

Shryock et al (1998) A2A-adenosine receptor reserve for coronary vasodilation. Circulation 98 711 PMID: 9715864

Komaki et al (2012) Trk and cAMP-dependent survival activity of adenosine A(2A) agonist CGS21680 on rat motoneurons in culture. Neurosci.Lett. 522 21 PMID: 22691937

If you know of a relevant reference for CGS 21680 hydrochloride, please let us know.

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Keywords: CGS 21680 hydrochloride, CGS 21680 hydrochloride supplier, A2A, agonists, Receptors, adenosines, CGS21680, hydrochloride, huntingtin, huntingtons, proliferation, neural, progenitor, cells, TrkB, anti-inflammatory, neuroprotective, Adenosine, Stem, Cell, Proliferation, 1063, Tocris Bioscience

75 Citations for CGS 21680 hydrochloride

Citations are publications that use Tocris products. Selected citations for CGS 21680 hydrochloride include:

Carlström et al (2011) Adenosine A2A receptor activation attenuates tubuloglomerular feedback responses by stimulation of endothelial nitric oxide synthase. Am J Physiol Renal Physiol 300 F457 PMID: 21106859

Su et al (2011) Receptor desensitization and blockade of the suppressive effects of prostaglandin E(2) and adenosine on the cytotoxic activity of human melanoma-infiltrating T lymphocytes. Cancer Immunol Immunother 60 111 PMID: 20960188

Ru et al (2011) Adenosine-induced activation of esophageal nociceptors. Am J Physiol Gastrointest Liver Physiol 300 G485 PMID: 21148396

Garcia et al (2008) Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis. J Neuroinflammation 22 445 PMID: 17898087

Shen et al (2008) Dichotomous DArgic control of striatal synaptic plasticity. Science 321 848 PMID: 18687967

Ruby et al (2014) Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light. Kidney Int 39 2432 PMID: 24755889

Caiazzo et al (2016) Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide. Biochem.Pharmacol. 112 72 PMID: 27188793

Ohta et al (2009) A2A adenosine receptor may allow expansion of T cells lacking effector functions in extracellular adenosine-rich microenvironments. Eur J Immunol 183 5487 PMID: 19843934

Ezeamuzie and Philips (1999) Adenosine A3 receptors on human eosinophils mediate inhibition of degranulation and superoxide anion release. Br J Pharmacol 127 188 PMID: 10369472

Bao et al (2013) Pannexin 1 channels link chemoattractant receptor signaling to local excitation and global inhibition responses at the front and back of polarized neutrophils. J Biol Chem 288 22650 PMID: 23798685

Loram et al (2013) Intrathecal injection of adenosine 2A receptor agonists reversed neuropathic allodynia through protein kinase (PK)A/PKC signaling. Brain Behav Immun 33 112 PMID: 23811314

Garção et al (2013) Functional interaction between pre-synaptic α6β2-containing nicotinic and adenosine A2A receptors in the control of DA release in the rat striatum. Br J Pharmacol 169 1600 PMID: 23638679

Yang et al (2013) Adenosine A2A receptor contributes to ischemic brain damage in newborn piglet. J Cereb Blood Flow Metab 33 1612 PMID: 23860373

Kiebala and Maggirwar (2011) Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency virus-1 Tat-mediated activation of microglial cells. PLoS One 6 e18633 PMID: 21494611

Xi et al (2009) Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol 47 684 PMID: 19695259

Epperson et al (2009) Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts. Am J Physiol Cell Physiol 296 C1171 PMID: 19244482

Perez-Aso et al (2015) Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther 17 249 PMID: 26370839

Eusemann et al (2015) Adenosine Receptors Differentially Regulate the Expression of Regulators of G-Protein Signalling (RGS) 2, 3 and 4 in Astrocyte-Like Cells. PLoS One 10 e0134934 PMID: 26263491

Kong et al (2019) Adenosine A2a receptor agonist CGS21680 treatment attenuates cardiopulmonary bypass-associated inflammatory lung injury in juvenile rats. Mol.Med.Rep. 20 117 PMID: 31115565

Nieri et al (2001) Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO. Br J Pharmacol 134 745 PMID: 11606314

Lee (2013) Both MC5r and A2Ar are required for protective regulatory immunity in the spleen of post-experimental autoimmune uveitis in mice. J Immunol 191 4103 PMID: 24043903

Pugliese et al (2009) The adenosine A2A receptor antagonist ZM241385 enhances neuronal survival after oxygen-glucose deprivation in rat CA1 hippocampal slices. Br J Pharmacol 157 818 PMID: 19422385

Xu et al (2022) Adenosine A2A receptors control synaptic remodeling in the adult brain. Sci Rep 12 14690 PMID: 36038626

Monticone et al (2022) Targeting the Cbl-b-Notch1 axis as a novel immunotherapeutic strategy to boost CD8+ T-cell responses. Front.Immunol. 13 987298 PMID: 36090975

Kornerup et al (2005) Pharmacological characterisation of the adenosine receptor mediating increased ion transport in the mouse isolated trachea and the effect of allergen challenge. Br J Pharmacol 144 1011 PMID: 15685200

Germack and Dickenson (2004) Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes. Br J Pharmacol 141 329 PMID: 14751870

Chen et al (2014) 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 J Neurosci 34 9621 PMID: 25031403

Nuccio et al (2019) Adenosine A2A receptor stimulation restores cell functions and differentiation in Niemann-Pick type C-like oligodendrocytes. Sci Rep 9 9782 PMID: 31278313

Hobson et al (2012) Stimulation of adenosine receptors in the nucleus accumbens reverses the expression of cocaine sensitization and cross-sensitization to DA D2 receptors in rats. Neuropharmacology 63 1172 PMID: 22749927

Park et al (2012) Proximal tubule sphingosine kinase-1 has a critical role in A1 adenosine receptor-mediated renal protection from ischemia. Kidney Int 82 878 PMID: 22695326

Yang et al (2006) The A2B adenosine receptor protects against inflammation and excessive vascular adhesion. J Clin Invest 116 1913 PMID: 16823489

Keir et al (2006) Mechanism of adenosine-induced airways obstruction in allergic guinea pigs. Br J Pharmacol 147 720 PMID: 16432507

O'Neill et al (2014) Persistent reduction of cocaine seeking by pharmacological manipulation of adenosine A1 and A 2A receptors during extinction training in rats. Psychopharmacology (Berl) 231 3179 PMID: 24562064

Das et al (2010) Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2A adenosine receptor agonists. J Nanobiotechnology 8 11 PMID: 20478037

Keene et al (2010) Multivalent dendrimeric and monomeric adenosine agonists attenuate cell death in HL-1 mouse cardiomyocytes expressing the A(3) receptor. Biochem Pharmacol 80 188 PMID: 20346920

Higley and Sabatini (2010) Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors. Nat Neurosci 13 958 PMID: 20601948

Gebremedhin et al (2010) Adenosine can mediate its actions through generation of reactive oxygen species. J Cereb Blood Flow Metab 30 1777 PMID: 20531463

Hiranita et al (2010) Reinforcing effects of sigma-receptor agonists in rats trained to self-administer cocaine. J Pharmacol Exp Ther 332 515 PMID: 19892920

Garavaglia et al (2010) Adaptation of NS cells growth and differentiation to high-throughput screening-compatible plates. BMC Neurosci 11 7 PMID: 20085655

Zhou et al (2010) GSK-3alpha directly regulates beta-adrenergic signaling and the response of the heart to hemodynamic stress in mice. J Clin Invest 120 2280 PMID: 20516643

Ferreira et al (2015) Presynaptic adenosine A2A receptors dampen cannabinoid CB1 receptor-mediated inhibition of corticostriatal glutamatergic transmission. Br J Pharmacol 172 1074 PMID: 25296982

Mills et al (2012) Extracellular adenosine signaling induces CX3CL1 expression in the brain to promote experimental autoimmune encephalomyelitis. J Neurochem 9 193 PMID: 22883932

Fernández-Dueñas et al (2012) Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R. J Immunol 123 373 PMID: 22924752

Jeon et al (2012) Oroxylin A Induces BDNF Expression on Cortical Neurons through Adenosine A2A Receptor Stimulation: A Possible Role in Neuroprotection. Neurochem Int 20 27 PMID: 24116271

O'Neill et al (2012) Adenosine A2A receptors in the nucleus accumbens bi-directionally alter cocaine seeking in rats. Neuropsychopharmacology 37 1245 PMID: 22169945

Kan et al (2012) Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. J Virol 86 10338 PMID: 22787201

Lee et al (2012) When cytokinin, a plant hormone, meets the adenosine A2A receptor: a novel neuroprotectant and lead for treating neurodegenerative disorders? PLoS One 7 e38865 PMID: 22719969

Mediero et al (2012) Adenosine A2A receptor activation prevents wear particle-induced osteolysis. Sci Transl Med 4 135ra65 PMID: 22623741

Nowak et al (2010) The A2aR adenosine receptor controls cytokine production in iNKT cells. Neuropharmacology 40 682 PMID: 20039304

Wang et al (2010) Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drug candidate ZM241385. Biomol Ther (Seoul) 5 e13883 PMID: 21079735

Kavanagh et al (2015) Role of adenosine receptor subtypes in metha. reward and reinforcement. J Neurogenet 89 265 PMID: 25301277

Kermanian et al (2015) Effects of adenosine A2a receptor agonist and antagonist on cerebellar nuclear factor-kB expression preceded by MDMA toxicity. Eneuro 28 120 PMID: 25678999

Polito et al (2015) Selective Effects of PDE10A Inhibitors on Striatopallidal Neurons Require Phosphatase Inhibition by DARPP-32(1,2,3). Mol Cell Biol 2 PMID: 26465004

Tosolini et al (2015) Human monocyte recognition of adenosine-based cyclic dinucleotides unveils the A2a Gαs protein-coupled receptor tonic inhibition of mitochondrially induced cell death. Psychopharmacology (Berl) 35 479 PMID: 25384972

Wydra et al (2015) On the role of A2A and D2 receptors in control of cocaine and food-seeking behaviors in rats. Am J Respir Cell Mol Biol 232 1767 PMID: 25420611

Li et al (2014) Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina. Vis Neurosci 31 237 PMID: 24844306

Welihinda and Amento (2014) Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation. J Inflamm (Lond) 11 37 PMID: 25473378

Ziemlinska et al (2014) Overexpression of BDNF increases excitability of the lumbar spinal network and leads to robust early locomotor recovery in completely spinalized rats. PLoS One 9 e88833 PMID: 24551172

Ahsan and Mehal (2014) Activation of adenosine receptor A2A increases HSC proliferation and inhibits death and senescence by down-regulation of p53 and Rb. Front Pharmacol 5 69 PMID: 24782773

Perígolo-Vicente et al (2014) IL-6, A1 and A2aR: a crosstalk that modulates BDNF and induces neuroprotection. Biochem Biophys Res Commun 449 477 PMID: 24845382

Fernández-Dueñas et al (2013) DA D(2) receptor-mediated modulation of adenosine A(2A) receptor agonist binding within the A(2A)R/D(2)R oligomer framework. FASEB J 63 42 PMID: 23619397

Aggarwal et al (2013) Macrophage A2A adenosinergic receptor modulates oxygen-induced augmentation of murine lung injury. Neuropsychopharmacology 48 635 PMID: 23349051

Garcia et al (2011) Adenosine A(2A) receptor activation prevents progressive kidney fibrosis in a model of immune-associated chronic inflammation. PLoS One 80 378 PMID: 21508927

Liu et al (2016) Activation of Adenosine 2A receptor inhibits neutrophil apoptosis in an autophagy-dependent manner in mice with systemic inflammatory response syndrome. Scientific Reports 6 33614 PMID: 27647162

Ledderose et al (2016) Adenosine arrests breast cancer cell motility by A3 receptor stimulation. Purinergic Signalling PMID: 27577957

Xiao et al (2013) Adenosine A2A receptor: a target for regulating renal interstitial fibrosis in obstructive nephropathy. PLoS One 8 e60173 PMID: 23585831

He et al (2013) Adenosine regulates bone metabolism via A1, A2A, and A2B receptors in bone marrow cells from normal humans and patients with multiple myeloma. FASEB J 27 3446 PMID: 23682121

Matos et al (2013) Antagonistic interaction between adenosine A2A receptors and Na+/K+-ATPase-α2 controlling glutamate uptake in astrocytes. J Neurosci 33 18492 PMID: 24259572

Wiseman et al (2013) Proteasomal degradation of eukaryotic elongation factor-2 kinase (EF2K) is regulated by cAMP-PKA signaling and the SCFβTRCP ubiquitin E3 ligase. J Biol Chem 288 17803 PMID: 23640883

Thomas et al (2013) Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. Bioorg Med Chem 21 7453 PMID: 24126093

Kozma et al (2013) Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor. Biochem Pharmacol 85 1171 PMID: 23376019

Núñez et al (2018) PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders. Front Pharmacol 9 1200 PMID: 30405415

Shifrut et al (2018) Genome-wide CRISPR Screens in Primary Human T Cells Reveal Key Regulators of Immune Function. Cell 175 1958 PMID: 30449619

Jain et al (2018) Melanotan II causes hypothermia in mice by activation of mast cells and stimulation of histamine 1 receptors. Am J Physiol Endocrinol Metab 315 E357 PMID: 29812984

Bakhshayesh et al (2017) The Mediating Role of A2A Adenosine Receptors in the Mitochondrial Pathway of Apoptotic Hippocampal Cell Death, Following the Administration of MDMA in Rat. Basic Clin Neurosci 8 317 PMID: 29158882

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Reviews for CGS 21680 hydrochloride

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HEK cell line expressing A2A Receptor.
By Tahmineh Safaie on 02/22/2021
Assay Type: In Vitro
Species: Human

HEK cell line expressing A2A Receptor were treated with CGS in presence or absence of ZM241385 for 30 minutes and level of cAMP was measured.

review image

works on inhibited CD4 cells.
By Anonymous on 06/05/2018
Assay Type: In Vitro
Species: Mouse

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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