Document Detail

Anticonvulsant properties of 3-hydroxy-2-quinoxalinecarboxylic acid, a newly found antagonist of excitatory amino acids.
MedLine Citation:
PMID:  2861099     Owner:  NLM     Status:  MEDLINE    
Various aromatic acids have been investigated as putative ligands of excitatory amino acid receptors. 3-Hydroxy-2-quinoxalinecarboxylic acid (HQC), at 1 mM, was found to antagonize the 22Na+ efflux produced in 22Na+-preloaded brain slices by N-methyl-D-aspartate and kainate. The response to glutamate was also affected but not that to quisqualate. The apparent KI value of HQC for suppression of the N-methyl-D-aspartate response was 0.27 mM. The anticonvulsant action of HQC was investigated in mice and rats. HQC administered intracerebroventricularly caused a dose dependent delay in the occurrence of picrotoxin induced convulsions and afforded protection against picrotoxin induced death. These results confirm the proposition that antagonists of excitatory amino acids possess anticonvulsant properties.
U Erez; H Frenk; O Goldberg; A Cohen; V I Teichberg
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of pharmacology     Volume:  110     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1985 Mar 
Date Detail:
Created Date:  1985-07-31     Completed Date:  1985-07-31     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  31-9     Citation Subset:  IM    
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MeSH Terms
Anticonvulsants / pharmacology*
Aspartic Acid / analogs & derivatives*,  antagonists & inhibitors
Glutamates / antagonists & inhibitors*
Glutamic Acid
Kainic Acid / antagonists & inhibitors*
Mice, Inbred Strains
Pyrrolidines / antagonists & inhibitors*
Quinoxalines / pharmacology*
Rats, Inbred Strains
Receptors, N-Methyl-D-Aspartate
Receptors, Neurotransmitter / drug effects
Sodium / metabolism
Structure-Activity Relationship
Reg. No./Substance:
0/Anticonvulsants; 0/Glutamates; 0/Pyrrolidines; 0/Quinoxalines; 0/Receptors, N-Methyl-D-Aspartate; 0/Receptors, Neurotransmitter; 1204-75-7/3-hydroxy-2-quinoxalinecarboxylic acid; 124-87-8/Picrotoxin; 487-79-6/Kainic Acid; 56-84-8/Aspartic Acid; 56-86-0/Glutamic Acid; 6384-92-5/N-Methylaspartate; 7440-23-5/Sodium

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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