GYKI 52466 dihydrochloride

Cat. No. 1454

GYKI 52466 dihydrochloride C17H15N3O2.2HCl [102771-26-6]

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Chemical Name: 4-(8-Methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine dihydrochloride

Biological Activity

Selective non-competitive 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. Also available as part of the AMPA Receptor Tocriset™. Also available as part of the Kainate Receptor Tocriset™.

Technical Data

M.Wt:
366.24
Formula:
C17H15N3O2.2HCl
Solubility:
Soluble to 50 mM in DMSO and to 10 mM in water
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
102771-26-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Rzeski et al (2001) Glutamate antagonists limit tumor growth. Proc.Natl.Acad.Sci.USA 98 6372. PMID: 11331750.

Szabados et al (2001) Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res.Bull. 55 387. PMID: 11489346.

Paternain et al (1995) Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons. Neuron 14 185. PMID: 7826635.

Donevan and Rogawsk (1993) GYKI 52466, a 2,3-benzodiazepine, is a highly selective, non-competitive antagonist of AMPA/kainate receptor responses. Neuron 10 51. PMID: 7678966.

Tarnawa et al (1989) Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466. Eur.J.Pharmacol. 167 193. PMID: 2574112.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for GYKI 52466 dihydrochloride include:

Fernandes et al (2014) In vitro ischemia triggers a transcriptional response to down-regulate synaptic proteins in hippocampal neurons. PLoS One 9 e99958. PMID: 24960035.

Kopach et al (2011) Inflammation alters trafficking of extrasynaptic AMPA receptors in tonically firing lamina II neurons of the rat spinal dorsal horn. Pain 152 912. PMID: 21282008.

Lobb et al (2010) A dynamic role for GABA receptors on the firing pattern of midbrain dopaminergic neurons. J Neurophysiol 104 403. PMID: 20445035.

Fritsch et al (2009) Pathological alterations in GABAergic interneurons and reduced tonic inhibition in the basolateral amygdala during epileptogenesis. Neuroscience 163 415. PMID: 19540312.

Lebrun-Julien et al (2009) Excitotoxic death of retinal neurons in vivo occurs via a non-cell-autonomous mechanism. J Neurosci 29 5536. PMID: 19403821.

Santos et al (2009) Transmission efficacy and plasticity in glutamatergic synapses formed by excitatory interneurons of the substantia gelatinosa in the rat spinal cord. PLoS One 4 e8047. PMID: 19956641.

Du et al (2008) The role of hippocampal GluR1 and GluR2 receptors in manic-like behavior. J Neurosci 28 68. PMID: 18171924.

Lin et al (2008) Integrin regulation of cytoplasmic calcium in excitatory neurons depends upon glutamate receptors and release from intracellular stores. J Pharmacol Exp Ther 37 770. PMID: 18289871.

Huang et al (2004) Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons. J Neurosci 24 4551. PMID: 15140926.

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Keywords: GYKI 52466 dihydrochloride, supplier, Selective, non-competitive, AMPA, antagonists, Glutamate, Receptors, iGlur, Ionotropic, GYKI52466, dihydrochloride, Tocris Bioscience, AMPA Receptor Antagonist products

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