SYM 2206
Chemical Name: (±)-4-(4-Aminophenyl)-1,2-dihydro-1-methyl-2-propylcarbamoyl-6,7-methylenedioxyphthalazine
Purity: ≥99%
Biological Activity
Novel, potent, non-competitive AMPA receptor antagonist (IC50 = 2.8 μM ). Acts allosterically at the same regulatory site as GYKI 52466 (Cat. No. 1454) and GYKI 53655 (Cat. No. 2555) and other benzodiazepines but does not bind to the central diazepine binding site. Selective for AMPA relative to kainate receptor sub-types. Similar potency to GYKI 53655. Anticonvulsant in vivo.Technical Data
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.
Additional Information
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Kainate receptor agonists, antagonists and allosteric modulators.
Bleakman et al.
Curr.Pharm.Des., 2002;8:873 -
Substituted 1,2-dihydrophthalazines: potent, selective and non-competitive inhibitors of the AMPA receptor.
Pelletier et al.
J.Med.Chem., 1996;39:343 -
Kainate-receptor-mediated sensory synaptic transmission in mammalian spinal cord.
Li et al.
Nature, 1999;397:161
Product Datasheets
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Citations for SYM 2206
The citations listed below are publications that use Tocris products. Selected citations for SYM 2206 include:
7 Citations: Showing 1 - 7
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Melanoma brain colonization involves the emergence of a brain-adaptive phenotype.
Authors: Nygaard Et al.
J Neurophysiol 2015;1:82
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Fast oscillatory activity in the anterior cingulate cortex: DArgic modulation and effect of perineuronal net loss.
Authors: Steullet Et al.
Front Cell Neurosci 2014;8:244
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Fast oscillatory activity induced by kainate receptor activation in the rat basolateral amygdala in vitro.
Authors: Randall Et al.
Eur J Neurosci 2011;33:914
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Inflammation alters trafficking of extrasynaptic AMPA receptors in tonically firing lamina II neurons of the rat spinal dorsal horn.
Authors: Kopach Et al.
Pain 2011;152:912
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Cholinergic neuromodulation controls directed temporal communication in neocortex in vitro.
Authors: Roopun Et al.
Front Neural Circuits 2010;4:8
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Characterization of AMPA receptors targeted by the climbing fiber transmitter mediating presynaptic inhibition of GABAergic transmission at cerebellar interneuron-Purkinje cell synapses.
Authors: Satake Et al.
J Neurosci 2006;26:2278
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Astrocyte-mediated activation of neuronal kainate receptors.
Authors: Liu Et al.
Oncoscience 2004;101:3172
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