Document Detail


4-Chloro-3-hydroxyanthranilate inhibits quinolinate production in the rat hippocampus in vivo.
MedLine Citation:
PMID:  8186995     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Quinolinic acid (QUIN) is a potential pathogen in a variety of excitotoxic and neuroviral brain diseases. In the present study, the ability of the QUIN synthesis inhibitor 4-chloro-3-hydroxyanthranilic acid to attenuate the production of QUIN was assessed in the hippocampus of awake rats. To this end, QUIN's immediate bioprecursor 3-hydroxyanthranilic acid (30 microM) was applied through a microdialysis probe, and QUIN production was monitored hourly in the perfusate. After 3 h, 4-chloro-3-hydroxyanthranilic acid (3 microM-3 mM) was included in the perfusion medium, and dialysis was continued for another 3 h. The drug caused dose-dependent inhibition of QUIN neosynthesis, with an apparent IC50 value of 32 microM. Discontinuation of drug administration, with continued perfusion of 3-hydroxyanthranilic acid, revealed that the drug effect was reversible. Intravenous application of 4-chloro-3-hydroxyanthranilic acid (14 mg/kg) resulted in a significant decrease in extracellular QUIN, reaching a nadir of 67% of saline-treated controls after 3 h. The data indicate that both intracerebral and systemic administration of 4-chloro-3-hydroxyanthranilic acid effectively interferes with QUIN production in the rat brain. The results suggest that QUIN synthesis inhibitors such as 4-chloro-3-hydroxyanthranilic acid may become of value in brain diseases that are caused by hyperphysiological quantities of QUIN.
Authors:
J L Walsh; H Q Wu; U Ungerstedt; R Schwarcz
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Brain research bulletin     Volume:  33     ISSN:  0361-9230     ISO Abbreviation:  Brain Res. Bull.     Publication Date:  1994  
Date Detail:
Created Date:  1994-06-21     Completed Date:  1994-06-21     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  7605818     Medline TA:  Brain Res Bull     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  513-6     Citation Subset:  IM    
Affiliation:
Maryland Psychiatric Research Center, University of Maryland School of Medicine, Baltimore 21228.
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MeSH Terms
Descriptor/Qualifier:
3-Hydroxyanthranilate 3,4-Dioxygenase
3-Hydroxyanthranilic Acid / analogs & derivatives*,  pharmacology
Animals
Dioxygenases*
Dose-Response Relationship, Drug
Extracellular Space / metabolism
Hippocampus / drug effects,  metabolism*
Male
Microdialysis
Oxygenases / antagonists & inhibitors
Quinolinic Acid / metabolism*
Rats
Rats, Sprague-Dawley
Grant Support
ID/Acronym/Agency:
NS 16102/NS/NINDS NIH HHS; NS 28236/NS/NINDS NIH HHS
Chemical
Reg. No./Substance:
23219-33-2/4-chloro-3-hydroxyanthranilic acid; 548-93-6/3-Hydroxyanthranilic Acid; 89-00-9/Quinolinic Acid; EC 1.13.-/Oxygenases; EC 1.13.11.-/Dioxygenases; EC 1.13.11.6/3-Hydroxyanthranilate 3,4-Dioxygenase

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


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