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GYKI 52466

GYKI 52466 is a 2,3-benzodiazepine that acts as an ionotropic glutamate receptor antagonist, which is a non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and 50 μM for AMPA-, kainate- and NMDA-induced responses respectively), orally-active anticonvulsant, and skeletal muscle relaxant. Unlike conventional 1,4-benzodiazepines, GYKI 52466 and related 2,3-benzodiazepines do not act on GABAA receptors. Like other AMPA receptor antagonists, GYKI 52466 has anticonvulsant and neuroprotective properties.

CNS review:

References

References

  1. (1998). "Allosteric regulation of α-amino-3-hydroxy-5-methyl-4-isoxazole-propionate receptors by thiocyanate and cyclothiazide at a common modulatory site distinct from that of 2,3-benzodiazepines". Neuroscience.
  2. (1993). "GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/Kainate receptor responses". Neuron.
  3. (1989). "Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466". European Journal of Pharmacology.
  4. (2001). "Glutamate antagonists limit tumor growth". Proceedings of the National Academy of Sciences.
  5. (1995). "Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons". Neuron.
  6. (2001). "Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655". Brain Research Bulletin.
  7. (March 1996). "2,3-Benzodiazepines (GYKI 52466 and Analogs): Negative Allosteric Modulators of AMPA Receptors". CNS Drug Reviews.
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ampa-receptor-antagonists anticonvulsants muscle-relaxants 4-aminophenyl-compounds
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