Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655

@article{Szabados2001ComparisonOA,
  title={Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655},
  author={Tam{\'a}s Szabados and G{\'a}bor Gigler and Istv{\'a}n Gacs{\'a}lyi and Istv{\'a}n Gyerty{\'a}n and Gy{\"o}rgy L{\'e}vay},
  journal={Brain Research Bulletin},
  year={2001},
  volume={55},
  pages={387-391}
}
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45 Citations
Highly Influential Citations
2
Background Citations
17
Methods Citations
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45 Citations

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Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.
TLDR
New cyclofunctionalized 2,3-benzodiazepines characterized by a triazolone or triazindione ring fused on the "c" edge of the heptatomic nucleus have been prepared and some of them proved to be more potent noncompetitive 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionate (AMPA) receptor antagonists.
Effect of two noncompetitive AMPA receptor antagonists GYKI 52466 and GYKI 53405 on vigilance, behavior and spike–wave discharges in a genetic rat model of absence epilepsy
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Heterocyclization of ethyl 2-acetyl(aroyl)-5-methylthieno[2,3-b]thiophene-3-acetates with hydrazine hydrate has been studied. A dependence of the reaction direaction on the nature of the substituent…
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Comparison of the AMPA Antagonist Action of New 2,3-Benzodiazepines in Vitro and Their Neuroprotective Effects in Vivo
TLDR
In vitro efficacy and in vivo neuroprotective action of new 2,3-benzodiazepine (2,3BDZ) AMPA antagonists have been compared for testing the hypothesis that blockade of AMPA receptors might result in significant protection of neurons against cellular damage.
SYNTHESE DE NOUVELLES 1,5-BENZODIAZEPINES ASSOCIANT DIFFERENTS HETEROCYCLES A CINQ CHAINONS
Nous décrivons la synthèse de nouvelles isoxazolinyl, pyrazolinyl, pyrazolyl et 1,2,3-triazolylméthylsulfanyl-1,5-benzodiazépines, ainsi que l'allylsulfanyl-1,2,4-triazolo-1,5-benzodiazépine par…
AMPA receptor antagonists as potential anticonvulsant drugs.
Over the last years alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid glutamate receptors (AMPARs) have been intensively studied owing to their crucial role in physiological and pathological…
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References

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GYKI 52466 and related 2,3-benzodiazepines as anticonvulsant agents in DBA/2 mice.
Non-N-methyl-D-aspartate receptor antagonism by 3-N-substituted 2,3-benzodiazepines: relationship to anticonvulsant activity.
TLDR
The increased affinity of the 3-N-substituted analogs relates to their increased binding and decreased unbinding rates, which are inversely correlated with increasing blocking potency.
The anticonvulsant effect of the non-NMDA antagonists, NBQX and GYKI 52466, in mice
GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses
Anticonvulsant actions of DS 103–282 Pharmacological studies in rodents and the baboon, Papio papio
Cerebroprotective Effect of a Non–N‐Methyl‐D‐Aspartate Antagonist, GYKI 52466, After Focal Ischemia in the Rat
TLDR
The cerebroprotective effect of GYKI 52466 in the rat suggests a possible therapeutic role for non-N-methyl-D-aspartate antagonists given shortly after the onset of stroke.
Investigations of non-NMDA receptor-induced toxicity in serum-free antioxidant-rich primary cultures of murine cerebellar granule cellsfn2 fn2 Abbreviations: AMPA, α amino-3-hydroxy-5-methyl-4-isoxazole propionate; CNQX, 6-Cyano-7-nitroquinoxaline-2,3-dione; div, days in vitro; GABA, γ-aminobu
Effects of the non‐NMDA antagonists NBQX and the 2,3‐benzodiazepine GYKI 52466 on different seizure types in mice: comparison with diazepam and interactions with flumazenil
TLDR
The data indicate that the GABAA receptor‐associated benzodiazepine site is not critically involved in anticonvulsant or adverse effects of GYKI 52466, and demonstrates that non‐NMDA antagonists lack a selective anticonVulsant action in standard models of generalized seizures.
Activity of 2,3-benzodiazepines at Native Rat and Recombinant Human Glutamate Receptors In Vitro: Stereospecificity and Selectivity Profiles
Effect of glutamate receptor antagonists on excitatory postsynaptic potentials in striatum
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