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γ-癸内酯对大鼠大脑皮层中谷氨酸结合的影响。

Effect of gamma-decanolactone on glutamate binding in the rat cerebral cortex.

作者信息

Pereira P, Elisabetsky E, Souza D O

机构信息

Departamento de Farmacologia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil.

出版信息

Neurochem Res. 1997 Dec;22(12):1507-10. doi: 10.1023/a:1021962714034.

Abstract

Epilepsy is one of the most common neurological disorders. Even though antiepileptic drugs can afford a reasonably satisfactory treatment for 80% of diagnosed patients, chronic intractable epilepsy still affects a significant number of people and more effective and less harmful antiepileptic drugs are needed. Previous studies have shown that gamma-decanolactone has dose-dependent sedative effects, including hypnotic, anticonvulsant and hypothermic properties in mice. The present study reports an inhibitory effect of gamma-decanolactone on glutamate binding (96.8% with 5 mM) in rat cortex membranes. The non competitive nature of glutamate binding inhibition as a neurochemical correlate of the anticonvulsant activity of gamma-decanolactone may be a relevant mode of action for further drug development.

摘要

癫痫是最常见的神经系统疾病之一。尽管抗癫痫药物能为80%的确诊患者提供较为令人满意的治疗,但慢性顽固性癫痫仍影响着相当一部分人,因此需要更有效且危害更小的抗癫痫药物。先前的研究表明,γ-癸内酯具有剂量依赖性镇静作用,包括在小鼠体内的催眠、抗惊厥和降温特性。本研究报告了γ-癸内酯对大鼠皮层膜中谷氨酸结合的抑制作用(5 mM时为96.8%)。谷氨酸结合抑制的非竞争性性质作为γ-癸内酯抗惊厥活性的神经化学关联,可能是进一步药物开发的一种相关作用模式。

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