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Quinoxalinediones: potent competitive non-NMDA glutamate receptor antagonists.
TLDR
Quinoxalinediones have been found to be potent and competitive antagonists at non-NMDA glutamate receptors and will be useful in the determination of the structure-activity relations of quisqualate and kainate receptors and the role of such receptors in synaptic transmission in the mammalian brain. Expand
Brain Glutamate Transporter Proteins Form Homomultimers*
TLDR
Chemical cross-linking is shown, followed by electrophoresis and immunoblotting, that three rat brain glutamate transporter proteins (GLAST, GLT and EAAC) form homomultimers, postulate that the glutamate transporters operate as homomULTimeric complexes. Expand
2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline: a neuroprotectant for cerebral ischemia.
TLDR
NBQX protects against global ischemia, even when administered 2 hours after an ischemic challenge, and is a potent and selective inhibitor of binding to the quisqualate subtype of the glutamate receptor, with no activity at the NMDA and glycine sites. Expand
Structure-activity relationships in the development of excitatory amino acid receptor agonists and competitive antagonists.
TLDR
The chemical features and SARs of agonists and antagonists, particularly those features associated with subtype selectivity, are described in this double-length review. Expand
The AMPA receptor antagonist NBQX has antiparkinsonian effects in monoamine‐depleted rats and MPTP‐treated monkeys
TLDR
Blockade of excitatory synaptic transmission by AMPA receptor antagonists may provide a new therapeutic strategy for Parkinson's disease (PD). Expand
New class of glutamate agonist structurally related to ibotenic acid
TLDR
A new class of Glu agonist obtained by structural manipulation of Ibo is described, which is likely to be converted by decarboxylation into muscimol20 during microelectrophoretic ejection near CNS neurones. Expand
The Binding of [3H]AMPA, a Structural Analogue of Glutamic Acid, to Rat Brain Membranes
TLDR
The result suggests that [3H]AMPA might represent binding to an excitatory GLU receptor, which is saturable and reversible at physiological pH and the highest blevel in striatal membranes. Expand
Synergism of the AMPA-antagonist NBQX and the NMDA-antagonist CPP with L-Dopa in models of Parkinson's disease
TLDR
Competitive NMDA and non-NMDA antagonists may offer a new therapeutic strategy for the treatment of Parkinson's disease through pharmacological blockade of overactive systems. Expand
Modulation of anxiety by β-carbolines and other benzodiazepine receptor ligands: Relationship of pharmacological to biochemical measures of efficacy
TLDR
Several beta-carbolines and other benzodiazepines (BZ) receptor ligands have been investigated for anxiolytic or anxiogenic action in 4 unrelated animal models of anxiety using rats and there was a quantitative relationship between the degree of enhancement of 35S-TBPS binding by a substance and its potency in the CDP cue test when such potency was expressed as numbers of BZ receptors occupied at the ED50 value in the pharmacological test. Expand
Calcium discriminates two [3H]kainate binding sites with different molecular target sizes in rat cortex
TLDR
The change in binding parameters of the two sites with radiation dose strongly suggests that low affinity, calcium-insensitive [3H]kainate binding sites are equivalent to quisqualate sites. Expand
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