Literature DB >> 2847085

6,7-Dichloro-3-hydroxy-2-quinoxalinecarboxylic acid is a relatively potent antagonist at NMDA and kainate receptors.

P Frey1, D Berney, P L Herrling, W Mueller, S Urwyler.   

Abstract

The 6,7-dichloro derivative of 3-hydroxy-2-quinoxalinecarboxylic acid (diCl-HQC) is a relatively potent antagonist at the two excitatory amino acid receptor subtypes activated by N-methyl-D-aspartate (NMDA) and kainic acid. It antagonizes NMDA-induced excitation in the frog spinal cord (pA2 5.8), i.e. with a potency similar to D-2-amino-7-phosphonoheptanoate (D-AP-7). It also antagonizes NMDA-induced sodium efflux from rat brain slices (pA2 5.6). The compound inhibits kainic acid-induced sodium efflux from rat brain slices with a pA2 of 5.4 and it inhibits [3H]kainic acid binding to rat brain membranes with a pKi of 5.4. DiCl-HQC is only weakly active at the quisqualate receptor. This spectrum of activities may make this compound a useful tool to investigate the pharmacology of excitatory amino acid receptors.

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Year:  1988        PMID: 2847085     DOI: 10.1016/0304-3940(88)90767-7

Source DB:  PubMed          Journal:  Neurosci Lett        ISSN: 0304-3940            Impact factor:   3.046


  2 in total

1.  A comparison of non-NMDA receptor channels in type-2 astrocytes and granule cells from rat cerebellum.

Authors:  D J Wyllie; S G Cull-Candy
Journal:  J Physiol       Date:  1994-02-15       Impact factor: 5.182

2.  Quinoxalines interact with the glycine recognition site of NMDA receptors: studies in guinea-pig myenteric plexus and in rat cortical membranes.

Authors:  D E Pellegrini-Giampietro; A Galli; M Alesiani; G Cherici; F Moroni
Journal:  Br J Pharmacol       Date:  1989-12       Impact factor: 8.739

  2 in total

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