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Gostatin blocks physiological actions and binding of acidic amino acid in rat brain

, : Gostatin blocks physiological actions and binding of acidic amino acid in rat brain. Neuropharmacology 28(4): 429-432

Gostatin, an inhibitor of aspartate aminotransferases isolated from Streptomyces sumanensis NK-23, was tested as an antagonist of acidic amino acid-mediated responses in the in vitro hippocampal slice and of acidic amino acid binding. Gostatin blocked responses to N-methyl-aspartate more potently than responses to kainate, .alpha.-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) or L-glutamate. Gostatin also displaced N-methyl-D-aspartate-sensitive [3H]-L-glutamate binding (Ki = 22.0 .mu.M) more potently than [3H]-kainate binding. Gostatin appears to be a relatively nonselective acidic amino acid antagonist in the mammalian central nervous system.


PMID: 2546088

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