Chemical Name: 2-(2-Furanyl)-7-[3-(4-methoxyphenyl)propyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine
Biological ActivitySCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM). Blocks the cytoprotective effect of A2A agonist CGS-21680 (Cat.No. 1063).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A2A receptor system using positron emission tomography.
Todde et al.
Protective roles of adenosine A1, A2, and A3 receptors in skeletal muscle ischemia and reperfusion injury.
Zheng et al.
Am.J.Physiol.Heart Circ.Physiol., 2007;293:3685
Citations for SCH 442416
The citations listed below are publications that use Tocris products. Selected citations for SCH 442416 include:
11 Citations: Showing 1 - 10
PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders.
Authors: Núñez Et al.
Front Pharmacol 2018;9:1200
Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity.
Authors: Cheng Et al.
Expression of CD39 on Activated T Cells Impairs their Survival in Older Individuals.
Authors: Fang Et al.
Cell Rep 2016;14:1218
Expression of CD39 on activated T cells impairs their survival in older individuals.
Authors: Fang Et al.
Cell Rep. 2016;14:1218
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.
J Neurochem 2015;35:479
Adenosine transiently modulates stimulated DA release in the caudate-putamen via A1 receptors.
Authors: Ross and Venton
Exp Ther Med 2015;132:51
Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina.
Authors: Li Et al.
Vis Neurosci 2014;31:237
Cardiac myocyte-secreted cAMP exerts paracrine action via adenosine receptor activation.
Authors: Sassi Et al.
J Clin Invest 2014;124:5385
Effect of A(2A) receptor antagonist (SCH 442416) on the mRNA expression of glutamate aspartate transporter and glutamine synthetase in rat retinal Müller cells under hypoxic conditions in vitro.
Authors: Yu Et al.
Am J Physiol Renal Physiol 2012;3:803
A2A and A3 adenosine receptor expression in rheumatoid arthritis: upregulation, inverse correlation with disease activity score and suppression of inflammatory cytokine and metalloproteinase release.
Authors: Varani Et al.
Arthritis Res Ther 2011;13:R197
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
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