2-3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline has been researched along with Brain-Infarction* in 1 studies
1 other study(ies) available for 2-3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline and Brain-Infarction
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Novel alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor antagonists of 2,3-benzodiazepine type: chemical synthesis, in vitro characterization, and in vivo prevention of acute neurodegeneration.
Under pathophysiological conditions, alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor activation is considered to play a key role in several disorders of the central nervous system. In the search for AMPA receptor antagonists, the synthesis and pharmacological characterization of a series of novel compounds that are structurally related to GYKI 52466 (1), a well-known selective noncompetitive AMPA receptor antagonist, was performed. In vitro, 2,3-dimethyl-6-phenyl-12H-[1,3]dioxolo[4,5-h]imidazo[1,2-c][2,3]benzodiazepine (ZK 187638, 14a) antagonized the kainate-induced currents in cultured hippocampal neurons with an IC(50) of 3.4 microM in a noncompetitive fashion. When tested in a clinically predictive rat model of acute ischemic stroke, this noncompetitive AMPA receptor antagonist significantly reduced brain infarction, indicating that it is neuroprotective after permanent focal cerebral ischemia. Topics: Acute Disease; Animals; Benzodiazepines; Binding, Competitive; Brain Infarction; Cells, Cultured; Dioxoles; Hippocampus; In Vitro Techniques; Ischemic Attack, Transient; Kainic Acid; Male; Mice; Nerve Degeneration; Neuroprotective Agents; Patch-Clamp Techniques; Prosencephalon; Radioligand Assay; Rats; Rats, Inbred F344; Receptors, AMPA | 2005 |