Indole-2-carboxylates, novel antagonists of the N-methyl-D-aspartate (NMDA)-associated glycine recognition sites: In vivo characterization

@article{Rao1993Indole2carboxylatesNA,
  title={Indole-2-carboxylates, novel antagonists of the N-methyl-D-aspartate
 (NMDA)-associated glycine recognition sites: In vivo characterization},
  author={Tadimeti S Rao and Nancy M. Gray and Michael Scott Dappen and Julie A. Cler and Steven J. Mick and Mark R. Emmett and Smriti Iyengar and Joseph B. Monahan and Alex A. Cordi and Paul L. Wood},
  journal={Neuropharmacology},
  year={1993},
  volume={32},
  pages={139-147}
}
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Functional NMDA Antagonists

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References

SHOWING 1-10 OF 22 REFERENCES

Characterization of indole-2-carboxylate derivatives as antagonists of N-methyl-D-aspartate receptor activity at the associated glycine recognition site.

In vivo transient bilateral carotid artery occlusion experiments revealed that these indole-2-carboxylate derivatives were capable of reducing the damage typically associated with an ischemic insult in Mongolian gerbil hippocampal neurons.

Novel indole-2-carboxylates as ligands for the strychnine-insensitive N-methyl-D-aspartate-linked glycine receptor.

A series of indole-2-carboxylates were prepared and evaluated for their ability to inhibit the binding at the strychnine-insensitive glycine receptor that is associated with the NMDA-PCP-glycine…

7-Chlorokynurenic acid is a selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex.

  • J. KempA. Foster G. Woodruff
  • Biology, Chemistry
    Proceedings of the National Academy of Sciences of the United States of America
  • 1988
Findings indicate that the glycine modulatory site is functional in intact adult tissue and that 7-Cl KYNA should prove to be a selective tool for elucidating the involvement of this site in physiological and pathological events mediated by N-Me-D-Asp receptors.

Selectivity of quinoxalines and kynurenines as antagonists of the glycine site on N-methyl-D-aspartate receptors.

7-Cl-kyn selectively attenuated NMDA receptor-mediated epileptiform bursts in the CA1 region of hippocampal slices perfused with zero-Mg medium, without reducing the amplitude of the primary population spike, which indicates that the glycine site plays a role in epileptic bursting mediated by NMDA receptors in adult rat hippocampus.

Neuropharmacological characterization of 1-Aminocyclopropane-1-carboxylate and 1-Aminocyclobutane-1-carboxylate, Ligands of the N-Methyl-D-Aspartate-associated Glycine Receptor

CGS 19755, a selective and competitive N-methyl-D-aspartate-type excitatory amino acid receptor antagonist.

CGS 19755 (cis-4-phosphonomethyl-2-piperidine carboxylic acid) was found to be a potent, stereospecific inhibitor of N-methyl-D-aspartate (NMDA)-evokes, but not KCl-evoked, [3H] acetylcholine release from slices of the rat striatum, suggesting a competitive interaction with NMDA-type receptors.

In vivo antagonism of agonist actions at N-methyl-d-aspartate and N-methyl-d-aspartate-associated glycine receptors in mouse cerebellum: Studies of 1-hydroxy-3-aminopyrrolidone-2

6,7-Dinitro-quinoxaline-2,3-dion and 6-nitro,7-cyano-quinoxaline-2,3-dion antagonise responses to NMDA in the rat spinal cord via an action at the strychnine-insensitive glycine receptor.

HA-996 (1-hydroxy-3-aminopyrrolidone-2) selectively reduces N-methyl-d-aspartate (NMDA)-mediated brain damage

Indole-2-carboxylic acid: a competitive antagonist of potentiation by glycine at the NMDA receptor.

Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current, suggesting that NMDA alone is not sufficient for channel activation.