Abstract |
Hydroxybenzoic and phthalic acids and their related compounds were tested for inhibitory activity to brain glutamate decarboxylase. Of mono-, di-, and trihydroxybenzoic acids, gallic acid was the most inhibitory, giving 50% inhibition at a concentration of 0.17 mM. Dihydroxybenzoic acids were less inhibitory than the trihydroxyacids but more than monohydroxybenzoic acids. Of the phthalic acid-related compounds tested, 4,5-dihydroxyisophthalic acid was the most potent inhibitor, producing 50% inhibition at 0.61 microM. The inhibition of these compounds was competitive with respect to L-glutamate. The Ki values were 0.02, 1.2 and 4.9 microM for 4,5-dihydroxyisophthalic acid, 5-hydroxyisophthalic acid and gallic acid, respectively. When administered intraventricularly to mice, 4,5-dihydroxyisophthalic acid produced a significant decrease in the gamma-aminobutyric acid content of the brain, resulting in induction of convulsions.
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Authors | A Endo, N Kitahara |
Journal | The Journal of antibiotics
(J Antibiot (Tokyo))
Vol. 34
Issue 10
Pg. 1351-4
(Oct 1981)
ISSN: 0021-8820 [Print] England |
PMID | 7309626
(Publication Type: Journal Article)
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Chemical References |
- Hydroxybenzoates
- Phthalic Acids
- 4,5-dihydroxyisophthalic acid
- gamma-Aminobutyric Acid
- Carboxy-Lyases
- Glutamate Decarboxylase
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Topics |
- Animals
- Brain
(enzymology)
- Brain Chemistry
(drug effects)
- Carboxy-Lyases
(antagonists & inhibitors)
- Glutamate Decarboxylase
(antagonists & inhibitors)
- Hydroxybenzoates
(pharmacology)
- Mice
- Phthalic Acids
(pharmacology)
- Structure-Activity Relationship
- gamma-Aminobutyric Acid
(analysis)
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