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单胺和γ-氨基丁酸代谢以及二正丙基乙酸酯和乙醇胺-O-硫酸酯的抗惊厥作用

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

作者信息

Horton R W, Anlezark G M, Sawaya M C, Meldrum B S

出版信息

Eur J Pharmacol. 1977 Feb 21;41(4):387-97. doi: 10.1016/0014-2999(77)90259-x.

Abstract

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

摘要

研究了行为变化、癫痫反应以及脑单胺和γ-氨基丁酸(GABA)代谢的时间进程,这些研究与二正丙基乙酸(DPA)和乙醇胺-O-硫酸盐(EOS)对DBA/2小鼠声音诱导癫痫发作的抗惊厥作用相关。EOS(75或150μg,脑室内注射)后脑单胺代谢的变化与其抗惊厥作用无关。主要作用是抑制GABA转氨酶(抑制50 - 70%),导致脑GABA浓度增加2 - 4倍。DPA(400 - 600mg/kg,腹腔注射)后可见脑GABA浓度(最大增加36%)、5-羟吲哚乙酸(5HIAA,最大增加134%)和高香草酸(HVA,最大增加183%)升高。HVA和5HIAA升高的时间进程与抗惊厥作用不相关。使用单胺合成抑制剂(α-甲基-p-酪氨酸和对氯苯丙氨酸)消除这些升高并未改变DPA的抗惊厥作用。使用丙磺舒的实验表明,DPA后5HIAA和HVA的升高是由于抑制了它们从脑内的主动转运。

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