Chemical Name: 2-(2-Furanyl)-7-(2-phenylethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine
Biological ActivitySCH 58261 is a potent and selective A2A adenosine receptor competitive antagonist (Ki = 1.3 nM). Displays 323-, 53- and 100-fold selectivity over A1, A2B and A3 receptors, respectively. Reduces melanoma tumor growth and TGF-β levels in WT and P2X7R-null mice.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Binding of the radioligand [3H]-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatal membranes.
Zocchi et al.
Effects of A1 and A2A adenosine receptor ligands in mouse acute models of pain.
Bastia et al.
The A2A adenosine receptor mediates coronary vasodilation.
Belardinelli et al.
Citations for SCH 58261
The citations listed below are publications that use Tocris products. Selected citations for SCH 58261 include:
42 Citations: Showing 1 - 10
Adenosine A2A receptors control synaptic remodeling in the adult brain.
Authors: Xu Et al.
Sci Rep 2022;12:14690
A2A receptor contributes to tumor progression in P2X7 null mice.
Authors: De Marchi Et al.
Front.Cell Dev.Biol. 2022;10:876510
Functional roles of ST8SIA3-mediated sialylation of striatal DA D2 and adenosine A2A receptors.
Authors: Lin Et al.
Transl Psychiatry 2019;9:209
Blockade of microglial adenosine A2A receptor suppresses elevated pressure-induced inflammation, oxidative stress, and cell death in retinal cells.
Authors: Aires Et al.
Adenosine A2A Receptors in the Rat Prelimbic Medial Prefrontal Cortex Control Delay-Based Cost-Benefit Decision Making.
Authors: Leffa Et al.
Front Mol Neurosci 2019;11:475
Anti-Depressant Flu Reveals its Therapeutic Effect Via Astrocytes.
Authors: Kinoshita Et al.
Adenosine binds predominantly to adenosine receptor A1 subtype in astrocytes and mediates an immunosuppressive effect.
Authors: Liu Et al.
Brain Res 2018;1700:47
Prostaglandin E2-mediated adenosinergic effects on CD14+ cells: Self-amplifying immunosuppression in cancer.
Authors: Al-Taei Et al.
Dominant immunosuppression of dendritic cell function by prostate-cancer-derived exosomes.
Authors: Salimu Et al.
J Extracell Vesicles 2017;6:1368823
Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity.
Authors: Cheng Et al.
Osteoblastic Lrp4 promotes osteoclastogenesis by regulating ATP release and adenosine-A2AR signaling.
Authors: Xiong Et al.
J Cell Biol 2017;216:761
Presynaptic muscarinic acetylcholine autoreceptors (M1, M2 and M4 subtypes), adenosine receptors (A1 and A2A) and tropomyosin-related kinase B receptor (TrkB) modulate the developmental synapse elimination process at the neuromuscular junction.
Authors: Nadal Et al.
Cancer Biol Ther 2016;9:67
Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.
Authors: Zhu Et al.
Psychopharmacology (Berl) 2015;35:621
Effects of adenosine A2a receptor agonist and antagonist on cerebellar nuclear factor-kB expression preceded by MDMA toxicity.
Authors: Kermanian Et al.
J Neuroinflammation 2015;28:120
On the role of A2A and D2 receptors in control of cocaine and food-seeking behaviors in rats.
Authors: Wydra Et al.
Mol Brain 2015;232:1767
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
Application of BRET to monitor ligand binding to GPCRs.
Authors: Stoddart Et al.
Nat Methods 2015;12:661
Adenosine A2AR blockade prevents neuroinflammation-induced death of retinal ganglion cells caused by elevated pressure.
Authors: Madeira Et al.
J Neurosci 2015;12:115
Expression and characterization of purinergic receptors in rat middle meningeal artery-potential role in migraine.
Authors: Haanes and Edvinsson
Med J Islam Repub Iran 2014;9:e108782
Anti-CD39 and anti-CD73 antibodies A1 and 7G2 improve targeted therapy in ovarian cancer by blocking adenosine-dependent immune evasion.
Authors: Häusler Et al.
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
Homeostatic control of synaptic activity by endogenous adenosine is mediated by adenosine kinase.
Authors: Diógenes Et al.
Cereb Cortex 2014;24:67
Ecto-5'-nucleotidase (CD73)-mediated formation of adenosine is critical for the striatal adenosine A2A receptor functions.
Authors: Augusto Et al.
Proc Natl Acad Sci U S A 2013;33:11390
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
Opiate-induced changes in brain adenosine levels and narcotic drug responses.
Authors: Wu Et al.
J Neuroinflammation 2013;228:235
Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth.
Authors: Mediavilla-Varela Et al.
Am J Transl Res 2013;14:860
Pathway-specific modulation of nucleus accumbens in reward and aversive behavior via selective transmitter receptors.
Authors: Hikida Et al.
Nat Neurosci 2013;110:342
Extracellular adenosine signaling induces CX3CL1 expression in the brain to promote experimental autoimmune encephalomyelitis.
Authors: Mills Et al.
J Neurosci 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
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
Adenosine receptor signaling modulates permeability of the blood-brain barrier.
Authors: Carman Et al.
J Neurosci 2011;31:13272
Adenosine A2A and A2B receptors are both required for adenosine A1 receptor-mediated cardioprotection.
Authors: Zhan Et al.
Am J Physiol Heart Circ Physiol 2011;301:H1183
A(2A) adenosine receptor-mediated increase in coronary flow in hyperlipidemic APOE-knockout mice.
Authors: Teng and Mustafa
J Exp Pharmacol 2011;2011:59
Role of aberrant striatal DA D1 receptor/cAMP/protein kinase A/DARPP32 signaling in the paradoxical calming effect of amphetamine.
Authors: Napolitano Et al.
J Neurosci 2010;30:11043
Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors.
Authors: Higley and Sabatini
Nat Neurosci 2010;13:958
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
A2A adenosine receptor (AR) activation inhibits pro-inflammatory cytokine production by human CD4+ helper T cells and regulates Helicobacter-induced gastritis and bacterial persistence.
Authors: Alam Et al.
Mucosal Immunol 2009;2:232
The A2B adenosine receptor impairs the maturation and immunogenicity of dendritic cells.
Authors: Wilson Et al.
J Immunol 2009;182:4616
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
Paraxanthine, the primary metabolite of caffeine, provides protection against DArgic cell death via stimulation of ryanodine receptor channels.
Authors: Guerreiro Et al.
Mol Pharmacol 2008;74:980
Dichotomous DArgic control of striatal synaptic plasticity.
Authors: Shen Et al.
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