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:
  • Formula:
  • Solubility:
    Soluble to 50 mM in DMSO and to 10 mM in water
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
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
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