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The convulsant drugs 3-mercaptopropionate and methionine sulfoximine inhibitl-glutamate andl-aspartate binding to a hydrophobic protein fraction from rat cerebral cortex
Authors:Ulises C Sábato  Sara Fiszer de Plazas  Eduardo De Robertis
Institution:(1) Instituto de Biologia Celular Facultad de Medicina, Universidad de Buenos Aires, 1121 Buenos Aires, Argentina
Abstract:The action of the convulsant drugs, methionine sulfoximine (MSO), 3-mercaptopropionate (3-MP), megimide (MG), and allylglycine on the binding ofl-14C]aspartate,l-14C]glutamate and 14C]GABA to a hydrophobic protein fraction isolated from rat cerebral cortex was studied. Using the convulsant at 10–4 M concentration and the radioactive ligands at 10conint6 M the binding ofl-14C]glutamate was inhibited 60% by 3-MP and 40% by MSO, while MG and allylglycine had no effect. The binding ofl-14C]aspartate was inhibited 55%, and 10–20% by 3-MP and MSO, respectively, while MG and allylglycine had not effect. None of the drugs mentioned, except for a minimal inhibition by MG, altered the binding of 14C]GABA. Neither MSO nor 3-MP affected the high-affinity sites forl-14C]glutamate orl-14C]aspartate, but they had a strong inhibitory action on the medium affinity site. These results are discussed in relation to the possible mechanism of action of these drugs onl-glutamate andl-aspartate receptors.
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