Monoamine and GABA metabolism and the anticonvulsant action of DI-n-propylacetate and ethanolamine-O-sulphate

作者: Roger W. Horton , Gill M. Anlezark , M.Christina B. Sawaya , Brian S. Meldrum

DOI: 10.1016/0014-2999(77)90259-X

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摘要: Abstract The time course of changes in behaviour, seizure response and cerebral monoamine γ-aminobutyric acid (GABA) metabolism has been studied relation to the anticonvulsant actions di-n-propylacetic (DPA) ethanolamine-O-sulphate (EOS) on sound-induced seizures DBA/2 mice. Changes after EOS (75 or 150 μg, intracerebroventricularly) were not related its action. primary effect was GABA-transaminase inhibition (by 50–70%) leading a 2–4 fold increase GABA concentration. Increases brain concentration (maximally 36%), 5-hydroxyindoleacetic (5HIAA, maximally 134%) homovanillic (HVA, 183%) seen DPA (400–600 mg/kg, i.p.). increases HVA 5HIAA did correlate with effect. Elimination these by use inhibitors synthesis (α-methyl-p-tyrosine p-chlorophenylalanine) alter DPA. Experiments using probenecid suggested that result from their active transport out brain.

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