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[结构上与γ-氨基丁酸相近的药理物质对大鼠大脑皮质体外合成、代谢及膜转运系统的影响]

[Effects of pharmacological substances structurally close to gamma-aminobutyric acid on the synthesis, metabolism and membrane transport systems in the cerebral cortex of rats in vitro].

作者信息

Kovalev G I, Prikhozhan A V, Eremenko A V

出版信息

Farmakol Toksikol. 1986 Jul-Aug;49(4):19-22.

PMID:3758322
Abstract

Effects of pantogam (calcium homopantotenate), piracetam, phenibut (beta-phenyl-GABA), sodium hydroxybutyrate and sodium valproate (depakine) at concentrations of 100 and 500 microM on the activities of glutamic acid decarboxylase, GABA-transaminase, Na, K- and Mg-ATPases, synaptosomal uptake and K+-stimulated release of 3H-GABA were studied in vitro. None of the compounds influenced the 3H-GABA uptake and activity of Mg-ATPase. Piracetam and phenibut stimulated slightly Na, K-ATPase. Phenibut and hydroxybutyrate exerted the inhibitory effect on GABA-transaminase activity. Hydroxybutyrate produced a moderate decrease of 3H-GABA release and suppressed the activity of glutamic acid decarboxylase.

摘要

研究了泛多利(高泛酸钙)、吡拉西坦、苯乙胺(β-苯基-GABA)、羟基丁酸钠和丙戊酸钠(德巴金)在浓度为100和500微摩尔时对谷氨酸脱羧酶、GABA转氨酶、钠钾-ATP酶和镁-ATP酶活性、突触体摄取以及3H-GABA钾刺激释放的体外影响。这些化合物均未影响3H-GABA摄取和镁-ATP酶活性。吡拉西坦和苯乙胺对钠钾-ATP酶有轻微刺激作用。苯乙胺和羟基丁酸钠对GABA转氨酶活性有抑制作用。羟基丁酸钠使3H-GABA释放适度减少,并抑制谷氨酸脱羧酶活性。

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