Compounds > 2-3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline

2-3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline and Acute-Disease

2-3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline has been researched along with Acute-Disease* in 2 studies

Other Studies

2 other study(ies) available for 2-3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline and Acute-Disease

Article	Year
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. Journal of medicinal chemistry, 2005, Jul-14, Volume: 48, Issue:14 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
Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine. Journal of medicinal chemistry, 2002, Sep-26, Volume: 45, Issue:20 Amino diacid 3, a highly selective competitive GluR5 kainate receptor antagonist, exhibited high GluR5 receptor affinity and selectivity over other glutamate receptors. Its diethyl ester prodrug 4 was orally active in two models of migraine: the neurogenic dural plasma protein extravasation model and the nucleus caudalis c-fos expression model. These data suggest that a GluR5 kainate receptor antagonist might be an efficacious antimigraine therapy with a novel mechanism of action. Topics: Acute Disease; Administration, Oral; Animals; Biological Availability; Calcium; Carboxylic Acids; Cell Line; Disease Models, Animal; Dose-Response Relationship, Drug; Esters; Excitatory Amino Acid Antagonists; Humans; Isoquinolines; Migraine Disorders; Prodrugs; Radioligand Assay; Rats; Rats, Wistar; Receptors, Kainic Acid	2002

Article

Year

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.

Journal of medicinal chemistry, 2005, Jul-14, Volume: 48, Issue:14

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

Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.

Journal of medicinal chemistry, 2002, Sep-26, Volume: 45, Issue:20

Amino diacid 3, a highly selective competitive GluR5 kainate receptor antagonist, exhibited high GluR5 receptor affinity and selectivity over other glutamate receptors. Its diethyl ester prodrug 4 was orally active in two models of migraine: the neurogenic dural plasma protein extravasation model and the nucleus caudalis c-fos expression model. These data suggest that a GluR5 kainate receptor antagonist might be an efficacious antimigraine therapy with a novel mechanism of action.

Topics: Acute Disease; Administration, Oral; Animals; Biological Availability; Calcium; Carboxylic Acids; Cell Line; Disease Models, Animal; Dose-Response Relationship, Drug; Esters; Excitatory Amino Acid Antagonists; Humans; Isoquinolines; Migraine Disorders; Prodrugs; Radioligand Assay; Rats; Rats, Wistar; Receptors, Kainic Acid

2002