Gostatin blocks physiological actions and binding of acidic amino acids in rat brain.
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 (AMPA) or L-glutamate. Gostatin also displaced N-methyl-D-aspartate-sensitive [3H]-L-glutamate binding (Ki = 22.0 microM) more potently than [3H]-kainate binding. Gostatin appears to be a relatively nonselective acidic amino acid antagonist in the mammalian central nervous system.
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1Central Nervous System Diseases Research, G. D. Searle & Co., Chesterfield, Mo. 63198.
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D000596:Amino Acids / Q000378:metabolism*; D000600:Amino Acids, Dicarboxylic / Q000494:pharmacology*; D000818:Animals; D001219:Aspartate Aminotransferases / Q000037:antagonists & inhibitors*; D001667:Binding, Competitive; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D017459:Receptors, Amino Acid; D011956:Receptors, Cell Surface / Q000378:metabolism; D017981:Receptors, Neurotransmitter / Q000378:metabolism
D000596:Amino Acids; D000600:Amino Acids, Dicarboxylic; D017459:Receptors, Amino Acid; D011956:Receptors, Cell Surface; D017981:Receptors, Neurotransmitter; C042220:gostatin; D001219:Aspartate Aminotransferases