GYKI 52466 dihydrochloride
Chemical Name: 4-(8-Methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine dihydrochloride
Purity: ≥98%
Biological Activity
GYKI 52466 dihydrochloride is a selective noncompetitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >50 μM for AMPA-, kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant. Has anti-proliferative effects in transformed cells.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.
Background References
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Differential signalling and glutamate receptor compositions in the OFF bipolar cell types in the mouse retina
T Ichinose, CB Hellmer
J. Physiol. (Lond.), 2016;594(4):883-94. -
Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons.
Paternain et al.
Neuron, 1995;14:185 -
Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655.
Szabados et al.
Brain Res.Bull., 2001;55:387 -
GYKI 52466, a 2,3-benzodiazepine, is a highly selective, non-competitive antagonist of AMPA/kainate receptor responses.
Donevan and Rogawsk
Neuron, 1993;10:51 -
Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466.
Tarnawa et al.
Eur.J.Pharmacol., 1989;167:193 -
Glutamate antagonists limit tumor growth.
Rzeski et al.
Proc.Natl.Acad.Sci.USA, 2001;98:6372
Product Datasheets
Citations for GYKI 52466 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for GYKI 52466 dihydrochloride include:
18 Citations: Showing 1 - 10
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Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors.
Authors: Bretin Et al.
PLoS One 2017;12:e0184429
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The Prefrontal Dectin-1/AMPA Receptor Signaling Pathway Mediates The Robust and Prolonged Antidepressant Effect of Proteo-β-Glucan from Maitake.
Authors: Bao Et al.
Sci Rep 2016;6:28395
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Lentinan produces a robust antidepressant-like effect via enhancing the prefrontal Dectin-1/AMPA receptor signaling pathway
Authors: Bao Et al.
Behavioural Brain Research 2016;317:263
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3'-Deoxyadenosine (Cordycepin) Produces a Rapid and Robust Antidepressant Effect via Enhancing Prefrontal AMPA Receptor Signaling Pathway.
Authors: Li Et al.
Int J Neuropsychopharmacol 2016;19
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In vitro ischemia triggers a transcriptional response to down-regulate synaptic proteins in hippocampal neurons.
Authors: Fernandes Et al.
PLoS One 2014;9:e99958
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Nitric oxide modulates the temporal properties of the glutamate response in type 4 OFF bipolar cells.
Authors: Vielma Et al.
PLoS One 2014;9:e114330
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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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Antidepressant-like effects of an AMPA receptor potentiator under a chronic mild stress paradigm.
Authors: Farley Et al.
Int J Neuropsychopharmacol 2010;13:1207
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A dynamic role for GABA receptors on the firing pattern of midbrain DArgic neurons.
Authors: Lobb Et al.
J Neurophysiol 2010;104:403
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Transmission efficacy and plasticity in glutamatergic synapses formed by excitatory interneurons of the substantia gelatinosa in the rat spinal cord.
Authors: Santos Et al.
PLoS One 2009;4:e8047
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Role of spinal cord alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors in complete Freund's adjuvant-induced inflammatory pain.
Authors: Park Et al.
Mol Pain 2009;4:67
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Excitotoxic death of retinal neurons in vivo occurs via a non-cell-autonomous mechanism.
Authors: Lebrun-Julien Et al.
J Neurosci 2009;29:5536
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Pathological alterations in GABAergic interneurons and reduced tonic inhibition in the basolateral amygdala during epileptogenesis.
Authors: Fritsch Et al.
Neuroscience 2009;163:415
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Integrin regulation of cytoplasmic calcium in excitatory neurons depends upon glutamate receptors and release from intracellular stores.
Authors: Lin Et al.
J Pharmacol Exp Ther 2008;37:770
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The role of hippocampal GluR1 and GluR2 receptors in manic-like behavior.
Authors: Du Et al.
J Neurosci 2008;28:68
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AMPA receptor-dependent H2O2 generation in striatal medium spiny neurons but not DA axons: one source of a retrograde signal that can inhibit DA release.
Authors: Avshalumov Et al.
J Neurophysiol 2008;100:1590
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Glutaric acid and its metabolites cause apoptosis in immature oligodendrocytes: a novel mechanism of white matter degeneration in glutaryl-CoA dehydrogenase deficiency.
Authors: Gerstner Et al.
Pediatr Res 2005;57:771
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Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons.
Authors: Huang Et al.
J Neurosci 2004;24:4551
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We use GYKI 52466 dihydrochloride at 10uM to inhibit AMPA receptors during our electrophysiology experiments. This allows us to isolate and study the effects of manipulations on other glutamate receptors. In the set of experiments we used this product for we were examining Kainate receptor properties and so the GYKI was used in conjunction with an NMDAR antagonist.
