Catalog Number: 1454
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.
Background References
  1. 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
  2. Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons.
    Paternain et al.
    Neuron, 1995;14:185
  3. Glutamate antagonists limit tumor growth.
    Rzeski et al.
    Proc.Natl.Acad.Sci.USA, 2001;98:6372
  4. 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
  5. Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466.
    Tarnawa et al.
    Eur.J.Pharmacol., 1989;167:193
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GYKI 52466 dihydrochloride include:

10 Citations: Showing 1 - 10
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  1. 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
  2. In vitro ischemia triggers a transcriptional response to down-regulate synaptic proteins in hippocampal neurons.
    Authors: Fernandes Et al.
    PLoS One 2014;9:e99958
  3. 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
  4. A dynamic role for GABA receptors on the firing pattern of midbrain dopaminergic neurons.
    Authors: Lobb Et al.
    J Neurophysiol 2010;104:403
  5. 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
  6. Excitotoxic death of retinal neurons in vivo occurs via a non-cell-autonomous mechanism.
    Authors: Lebrun-Julien Et al.
    J Neurosci 2009;29:5536
  7. Pathological alterations in GABAergic interneurons and reduced tonic inhibition in the basolateral amygdala during epileptogenesis.
    Authors: Fritsch Et al.
    Neuroscience 2009;163:415
  8. 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
  9. The role of hippocampal GluR1 and GluR2 receptors in manic-like behavior.
    Authors: Du Et al.
    J Neurosci 2008;28:68
  10. 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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