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company name :
Tocris Bioscience
product type :
chemical
product name :
1063/10
catalog :
1063/10
quantity :
10 mg (also 50 mg)
price :
385 USD
more info or order :
citations: 84
Reference
Monticone G, Huang Z, Csibi F, Leit S, Ciccone D, Champhekar A, et al. Targeting the Cbl-b-Notch1 axis as a novel immunotherapeutic strategy to boost CD8+ T-cell responses. Front Immunol. 2022;13:987298 pubmed publisher
Xu X, Beleza R, Gon xe7 alves F, Valbuena S, Al xe7 ada Morais S, Gon xe7 alves N, et al. Adenosine A2A receptors control synaptic remodeling in the adult brain. Sci Rep. 2022;12:14690 pubmed publisher
De Nuccio C, Bernardo A, Ferrante A, Pepponi R, Martire A, Falchi M, et al. Adenosine A2A receptor stimulation restores cell functions and differentiation in Niemann-Pick type C-like oligodendrocytes. Sci Rep. 2019;9:9782 pubmed publisher
Kong X, Zuo Y, Huang Y, Ge J. Adenosine A2a receptor agonist CGS21680 treatment attenuates cardiopulmonary bypass‑associated inflammatory lung injury in juvenile rats. Mol Med Rep. 2019;20:117-124 pubmed publisher
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Nakashima K, Iwao K, Inoue T, Haga A, Tsutsumi T, Mochita M, et al. Stimulation of the adenosine A3 receptor, not the A1 or A2 receptors, promote neurite outgrowth of retinal ganglion cells. Exp Eye Res. 2018;170:160-168 pubmed publisher
Bakhshayesh M, Golab F, Kermanian F, Mehdizadeh M, Katebi A, Soleimani M, 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. Basic Clin Neurosci. 2017;8:317-324 pubmed publisher
Lee D, Preble J, Lee S, Foster C, Taylor A. MC5r and A2Ar Deficiencies During Experimental Autoimmune Uveitis Identifies Distinct T cell Polarization Programs and a Biphasic Regulatory Response. Sci Rep. 2016;6:37790 pubmed publisher
Liu Y, Yang T, Zhao L, Ni Z, Yang N, He F, et al. Activation of Adenosine 2A receptor inhibits neutrophil apoptosis in an autophagy-dependent manner in mice with systemic inflammatory response syndrome. Sci Rep. 2016;6:33614 pubmed publisher
Ledderose C, Hefti M, Chen Y, Bao Y, Seier T, Li L, et al. Adenosine arrests breast cancer cell motility by A3 receptor stimulation. Purinergic Signal. 2016;12:673-685 pubmed
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Polito M, Guiot E, Gangarossa G, Longueville S, Doulazmi M, Valjent E, et al. Selective Effects of PDE10A Inhibitors on Striatopallidal Neurons Require Phosphatase Inhibition by DARPP-32(1,2,3). Eneuro. 2015;2: pubmed publisher
Perez Aso M, Montesinos M, Mediero A, Wilder T, Schafer P, Cronstein B. Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther. 2015;17:249 pubmed publisher
Eusemann T, Willmroth F, Fiebich B, Biber K, van Calker D. Adenosine Receptors Differentially Regulate the Expression of Regulators of G-Protein Signalling (RGS) 2, 3 and 4 in Astrocyte-Like Cells. PLoS ONE. 2015;10:e0134934 pubmed publisher
Kermanian F, Soleimani M, Pourheydar B, Samzadeh Kermani A, Mohammadzadeh F, Mehdizadeh M. Effects of adenosine A2a receptor agonist and antagonist on cerebellar nuclear factor-kB expression preceded by MDMA toxicity. Med J Islam Repub Iran. 2014;28:120 pubmed
Welihinda A, Amento E. Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation. J Inflamm (Lond). 2014;11:37 pubmed publisher
Wydra K, Suder A, Borroto Escuela D, Filip M, Fuxe K. On the role of Aâ‚‚A and Dâ‚‚ receptors in control of cocaine and food-seeking behaviors in rats. Psychopharmacology (Berl). 2015;232:1767-78 pubmed publisher
Tosolini M, Pont F, Bétous D, Ravet E, Ligat L, Lopez F, et al. Human monocyte recognition of adenosine-based cyclic dinucleotides unveils the A2a Gαs protein-coupled receptor tonic inhibition of mitochondrially induced cell death. Mol Cell Biol. 2015;35:479-95 pubmed publisher
Kavanagh K, Schreiner D, Levis S, O Neill C, Bachtell R. Role of adenosine receptor subtypes in methamphetamine reward and reinforcement. Neuropharmacology. 2015;89:265-73 pubmed publisher
Ferreira S, Gonçalves F, Marques J, Tomé Ã, Rodrigues R, Nunes Correia I, et al. Presynaptic adenosine A2A receptors dampen cannabinoid CB1 receptor-mediated inhibition of corticostriatal glutamatergic transmission. Br J Pharmacol. 2015;172:1074-86 pubmed publisher
Chen Z, Xiong C, Pancyr C, Stockwell J, Walz W, Cayabyab F. 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 re. J Neurosci. 2014;34:9621-43 pubmed publisher
Persson P, Hansell P, Palm F. Reduced adenosine A2a receptor-mediated efferent arteriolar vasodilation contributes to diabetes-induced glomerular hyperfiltration. Kidney Int. 2015;87:109-15 pubmed publisher
Perígolo Vicente R, Ritt K, Gonçalves de Albuquerque C, Castro Faria Neto H, Paes de Carvalho R, Giestal de Araujo E. IL-6, A1 and A2aR: a crosstalk that modulates BDNF and induces neuroprotection. Biochem Biophys Res Commun. 2014;449:477-82 pubmed publisher
Li H, Chuang A, O BRIEN J. Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina. Vis Neurosci. 2014;31:237-43 pubmed publisher
Ahsan M, Mehal W. Activation of adenosine receptor A2A increases HSC proliferation and inhibits death and senescence by down-regulation of p53 and Rb. Front Pharmacol. 2014;5:69 pubmed publisher
Ruby C, Vadnie C, Hinton D, Abulseoud O, Walker D, O Connor K, et al. Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light. Neuropsychopharmacology. 2014;39:2432-40 pubmed publisher
O Neill C, Hobson B, Levis S, Bachtell R. Persistent reduction of cocaine seeking by pharmacological manipulation of adenosine A1 and A 2A receptors during extinction training in rats. Psychopharmacology (Berl). 2014;231:3179-88 pubmed publisher
Ziemli ska E, K gler S, Schachner M, Wewi r I, Czarkowska Bauch J, Skup M. Overexpression of BDNF increases excitability of the lumbar spinal network and leads to robust early locomotor recovery in completely spinalized rats. PLoS ONE. 2014;9:e88833 pubmed publisher
Subramanian M, Kini R, Madasu M, Ohta A, Nowak M, Exley M, et al. Extracellular adenosine controls NKT-cell-dependent hepatitis induction. Eur J Immunol. 2014;44:1119-29 pubmed publisher
Ouyang X, Ghani A, Malik A, Wilder T, COLEGIO O, Flavell R, et al. Adenosine is required for sustained inflammasome activation via the A?A receptor and the HIF-1? pathway. Nat Commun. 2013;4:2909 pubmed publisher
Matos M, Augusto E, Agostinho P, Cunha R, Chen J. Antagonistic interaction between adenosine A2A receptors and Na+/K+-ATPase-?2 controlling glutamate uptake in astrocytes. J Neurosci. 2013;33:18492-502 pubmed publisher
Thomas R, Lee J, Chevalier V, Sadler S, Selesniemi K, Hatfield S, et al. Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. Bioorg Med Chem. 2013;21:7453-64 pubmed publisher
Jeon S, Bak H, Seo J, Han S, Lee S, Han S, et al. Oroxylin A Induces BDNF Expression on Cortical Neurons through Adenosine A2A Receptor Stimulation: A Possible Role in Neuroprotection. Biomol Ther (Seoul). 2012;20:27-35 pubmed publisher
Lee D, Taylor A. Both MC5r and A2Ar are required for protective regulatory immunity in the spleen of post-experimental autoimmune uveitis in mice. J Immunol. 2013;191:4103-11 pubmed publisher
Koscsó B, Csóka B, Kókai E, Németh Z, Pacher P, Virag L, et al. Adenosine augments IL-10-induced STAT3 signaling in M2c macrophages. J Leukoc Biol. 2013;94:1309-15 pubmed publisher
Yang Z, Wang B, Kwansa H, Heitmiller K, Hong G, Carter E, et al. Adenosine A2A receptor contributes to ischemic brain damage in newborn piglet. J Cereb Blood Flow Metab. 2013;33:1612-20 pubmed publisher
Loram L, Taylor F, Strand K, Harrison J, Rzasalynn R, Sholar P, et al. Intrathecal injection of adenosine 2A receptor agonists reversed neuropathic allodynia through protein kinase (PK)A/PKC signaling. Brain Behav Immun. 2013;33:112-22 pubmed publisher
Bao Y, Chen Y, Ledderose C, Li L, Junger W. 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. 2013;288:22650-7 pubmed publisher
He W, Mazumder A, Wilder T, Cronstein B. Adenosine regulates bone metabolism via A1, A2A, and A2B receptors in bone marrow cells from normal humans and patients with multiple myeloma. FASEB J. 2013;27:3446-54 pubmed publisher
Vincenzi F, Corciulo C, Targa M, Merighi S, Gessi S, Casetta I, et al. Multiple sclerosis lymphocytes upregulate A2A adenosine receptors that are antiinflammatory when stimulated. Eur J Immunol. 2013;43:2206-16 pubmed publisher
Wiseman S, Shimizu Y, Palfrey C, Nairn A. Proteasomal degradation of eukaryotic elongation factor-2 kinase (EF2K) is regulated by cAMP-PKA signaling and the SCF?TRCP ubiquitin E3 ligase. J Biol Chem. 2013;288:17803-11 pubmed publisher
Garção P, Szabó E, Wopereis S, Castro A, Tome A, Prediger R, et al. Functional interaction between pre-synaptic ?6?2-containing nicotinic and adenosine A2A receptors in the control of dopamine release in the rat striatum. Br J Pharmacol. 2013;169:1600-11 pubmed publisher
Fernández Dueñas V, Gómez Soler M, Morató X, Núñez F, Das A, Kumar T, et al. Dopamine D(2) receptor-mediated modulation of adenosine A(2A) receptor agonist binding within the A(2A)R/D(2)R oligomer framework. Neurochem Int. 2013;63:42-6 pubmed publisher
Xiao H, Shen H, Liu W, Xiong R, Li P, Meng G, et al. Adenosine A2A receptor: a target for regulating renal interstitial fibrosis in obstructive nephropathy. PLoS ONE. 2013;8:e60173 pubmed publisher
Kozma E, Gizewski E, Tosh D, Squarcialupi L, Auchampach J, Jacobson K. Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor. Biochem Pharmacol. 2013;85:1171-81 pubmed publisher
Aggarwal N, D Alessio F, Eto Y, Chau E, Avalos C, Waickman A, et al. Macrophage A2A adenosinergic receptor modulates oxygen-induced augmentation of murine lung injury. Am J Respir Cell Mol Biol. 2013;48:635-46 pubmed publisher
Fernández Dueñas V, Gómez Soler M, Jacobson K, Kumar S, Fuxe K, Borroto Escuela D, et al. Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R. J Neurochem. 2012;123:373-84 pubmed publisher
Moidunny S, Vinet J, Wesseling E, Bijzet J, Shieh C, Van IJzendoorn S, et al. Adenosine A2B receptor-mediated leukemia inhibitory factor release from astrocytes protects cortical neurons against excitotoxicity. J Neuroinflammation. 2012;9:198 pubmed
Mills J, Alabanza L, Mahamed D, Bynoe M. Extracellular adenosine signaling induces CX3CL1 expression in the brain to promote experimental autoimmune encephalomyelitis. J Neuroinflammation. 2012;9:193 pubmed
Kan Y, Okabayashi T, Yokota S, Yamamoto S, Fujii N, Yamashita T. Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. J Virol. 2012;86:10338-46 pubmed publisher
Hobson B, Merritt K, Bachtell R. Stimulation of adenosine receptors in the nucleus accumbens reverses the expression of cocaine sensitization and cross-sensitization to dopamine D2 receptors in rats. Neuropharmacology. 2012;63:1172-81 pubmed publisher
Lee Y, Yang Y, Huang C, Kuo T, Lin J, Yang D, et al. When cytokinin, a plant hormone, meets the adenosine A2A receptor: a novel neuroprotectant and lead for treating neurodegenerative disorders?. PLoS ONE. 2012;7:e38865 pubmed publisher
Park S, Kim M, Kim J, Brown K, Haase V, D Agati V, et al. Proximal tubule sphingosine kinase-1 has a critical role in A1 adenosine receptor-mediated renal protection from ischemia. Kidney Int. 2012;82:878-91 pubmed publisher
Mediero A, Frenkel S, Wilder T, He W, Mazumder A, Cronstein B. Adenosine A2A receptor activation prevents wear particle-induced osteolysis. Sci Transl Med. 2012;4:135ra65 pubmed publisher
Li N, Mu L, Wang J, Zhang J, Xie X, Kong Q, et al. Activation of the adenosine A2A receptor attenuates experimental autoimmune myasthenia gravis severity. Eur J Immunol. 2012;42:1140-51 pubmed publisher
O Neill C, Letendre M, Bachtell R. Adenosine A2A receptors in the nucleus accumbens bi-directionally alter cocaine seeking in rats. Neuropsychopharmacology. 2012;37:1245-56 pubmed publisher
Garcia G, Truong L, Chen J, Johnson R, Feng L. Adenosine A(2A) receptor activation prevents progressive kidney fibrosis in a model of immune-associated chronic inflammation. Kidney Int. 2011;80:378-88 pubmed publisher
Kiebala M, Maggirwar S. Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency virus-1 Tat-mediated activation of microglial cells. PLoS ONE. 2011;6:e18633 pubmed publisher
Ru F, Surdenikova L, Brozmanova M, Kollarik M. Adenosine-induced activation of esophageal nociceptors. Am J Physiol Gastrointest Liver Physiol. 2011;300:G485-93 pubmed publisher
Carlström M, Wilcox C, Welch W. Adenosine A2A receptor activation attenuates tubuloglomerular feedback responses by stimulation of endothelial nitric oxide synthase. Am J Physiol Renal Physiol. 2011;300:F457-64 pubmed publisher
Wang Z, Che P, Du J, Ha B, Yarema K. Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drug candidate ZM241385. PLoS ONE. 2010;5:e13883 pubmed publisher
Su Y, Jackson E, Gorelik E. 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. 2011;60:111-22 pubmed publisher
Higley M, Sabatini B. Competitive regulation of synaptic Ca2+ influx by D2 dopamine and A2A adenosine receptors. Nat Neurosci. 2010;13:958-66 pubmed publisher
Gebremedhin D, Weinberger B, Lourim D, Harder D. Adenosine can mediate its actions through generation of reactive oxygen species. J Cereb Blood Flow Metab. 2010;30:1777-90 pubmed publisher
Zhou J, Lal H, Chen X, Shang X, Song J, Li Y, et al. GSK-3alpha directly regulates beta-adrenergic signaling and the response of the heart to hemodynamic stress in mice. J Clin Invest. 2010;120:2280-91 pubmed publisher
Das A, Sanjayan G, Kecskés M, Yoo L, Gao Z, Jacobson K. Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2A adenosine receptor agonists. J Nanobiotechnology. 2010;8:11 pubmed publisher
Keene A, Balasubramanian R, Lloyd J, Shainberg A, Jacobson K. Multivalent dendrimeric and monomeric adenosine agonists attenuate cell death in HL-1 mouse cardiomyocytes expressing the A(3) receptor. Biochem Pharmacol. 2010;80:188-96 pubmed publisher
Garavaglia A, Moiana A, Camnasio S, Bolognini D, Papait R, Rigamonti D, et al. Adaptation of NS cells growth and differentiation to high-throughput screening-compatible plates. BMC Neurosci. 2010;11:7 pubmed publisher
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Hiranita T, Soto P, Tanda G, Katz J. Reinforcing effects of sigma-receptor agonists in rats trained to self-administer cocaine. J Pharmacol Exp Ther. 2010;332:515-24 pubmed publisher
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Xi J, McIntosh R, Shen X, Lee S, Chanoit G, Criswell H, et al. Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol. 2009;47:684-90 pubmed publisher
Pugliese A, Traini C, Cipriani S, Gianfriddo M, Mello T, Giovannini M, et al. The adenosine A2A receptor antagonist ZM241385 enhances neuronal survival after oxygen-glucose deprivation in rat CA1 hippocampal slices. Br J Pharmacol. 2009;157:818-30 pubmed publisher
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Garcia G, Truong L, Li P, Zhang P, Du J, Chen J, et al. Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis. FASEB J. 2008;22:445-54 pubmed
Yang D, Zhang Y, Nguyen H, Koupenova M, Chauhan A, Makitalo M, et al. The A2B adenosine receptor protects against inflammation and excessive vascular adhesion. J Clin Invest. 2006;116:1913-23 pubmed
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product information
master code :
1063
SKU :
1063/10
product name :
CGS 21680 hydrochloride
unit size :
10 mg (also 50 mg)
description :
A2A agonist
target :
Adenosine A2a Receptor Agonists
category :
Small Molecules
purity :
98%
observed molecular weight :
535.99
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
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).
top caption :
A2A agonist
extended description :
A2A agonist
chemical name text :
4-[2-[[6-Amino-9-(N-ethyl- -D-ribofuranuronamidosyl)-9H-purin-2-yl]amino]ethyl]benzenepropanoic acid hydrochloride
formula :
C23H29N7O6.HCl
formula text :
C23H29N7O6.HCl
cas num :
124431-80-7
USD :
385 USD
product details :
A2A agonist
storage :
Desiccate at -20░C
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK