GYKI 52466 explained

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.^{[1] [2] [3] [4]} Unlike conventional 1,4-benzodiazepines, GYKI 52466 and related 2,3-benzodiazepines do not act on GABA_A receptors.^[5] Like other AMPA receptor antagonists, GYKI 52466 has anticonvulsant and neuroprotective properties.^[6]

See also

• GYKI 52895, another 2,3-benzodiazepine with other than GABAergic function
• Tifluadom
• Lufuradom

Notes and References

1. 10.1016/s0306-4522(98)00109-2 . 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 . 1998 . Donevan . S.D . Rogawski . M.A . Neuroscience . 87 . 3 . 615–629 . 9758228 . 14817743 .
2. 10.1016/0896-6273(93)90241-i . GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/Kainate receptor responses . 1993 . Donevan . Sean D. . Rogawski . Michael A. . Neuron . 10 . 1 . 51–59 . 7678966 . 16011527 .
3. 10.1016/0014-2999(89)90579-7 . Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466 . 1989 . Tarnawa . István . Farkas . Sándor . Berzsenyi . Pál . Pataki . Ágnes . Andrási . Ferenc . European Journal of Pharmacology . 167 . 2 . 193–199 . 2574112 .
4. 10.1073/pnas.091113598 . Glutamate antagonists limit tumor growth . 2001 . Rzeski . W. . Turski . L. . Ikonomidou . C. . Proceedings of the National Academy of Sciences . 98 . 11 . 6372–6377 . 11331750 . 33475 . free .
5. 10.1016/0896-6273(95)90253-8 . Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons . 1995 . Paternain . Ana V. . Morales . Miguel . Lerma . Juan . Neuron . 14 . 1 . 185–189 . 7826635 . 6037517 . free .
6. 10.1016/s0361-9230(01)00516-0 . Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655 . 2001 . Szabados . Tamás . Gigler . Gábor . Gacsályi . István . Gyertyán . István . Lévay . György . Brain Research Bulletin . 55 . 3 . 387–391 . 11489346 . 23142293 .