CGS 21680 hydrochloride

Cat. No. 1063

CGS 21680 hydrochloride C23H29N7O6.HCl [124431-80-7]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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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.

If you know of a relevant reference for this product please let us know.

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

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

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

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.

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.

Kavanagh et al (2015) Role of adenosine receptor subtypes in methamphetamine 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.

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.

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.

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.

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

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.

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

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.

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

Fernández-Dueñas et al (2013) Dopamine 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.

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.

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.

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.

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

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.

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

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.

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.

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

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

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.

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.

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

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.

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.

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

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

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

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.

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.

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.

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.

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

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.

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.

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

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

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

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

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.

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.

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.

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