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Effect of γ-ethyl-γ-phenyl-butyrolactone (EFBL), anticonvulsant and hypnotic drug, on mouse brain catecholamine levels

机译:γ-乙基-γ-苯基-丁内酯(EFBL),抗惊厥药和催眠药对小鼠脑儿茶酚胺水平的影响

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摘要

γ-Ethyl-γ-phenyl-butyrolactone (EFBL) is a structural combination of the anticonvulsant γ-hydroxy-γ-ethyl-γ-phenylbutyramide (HEPB) and the hypnotic γ-butyrolactone (GBL), which inherits both properties. To clarify its mechanism of action, the effects of EFBL, GBL and HEPB on dopamine (DA) and noradrenaline (NA) brain levels were investigated. Influences of chlorpromazine, phenelzine and amino-oxyacetic acid were also studied. EFBL increased DA in a dose-dependent manner, remaining enhanced by 80 % over a period of 24 h and augmented NA by 54 % one hour after treatment. HEPB increased DA and NA approximately 2-fold after the first hour. GBL raised DA and NA after three and 24 h, resp. EFBL reversed chlorpromazine effects but potentiated those of phenelzine on DA. Amino-oxyacetic modified neither DA nor NA brain levels, not even in the presence of EFBL. The anticonvulsant and hypnotic properties of EFBL are attributed to its effect on presynaptic dopaminergic receptors and its lasting effect on ethyl and phenyl radicals that hinder its degradation. The results support the role of DA and NA in regulating seizure activity in the brain and indicate that EFBL offers a potential treatment for refractory epilepsy without complementary drugs and Parkinson’s disease, without the drawbacks of oral therapies.
机译:γ-乙基-γ-苯基丁内酯(EFBL)是抗惊厥性γ-羟基-γ-乙基-γ-苯基丁丁酰胺(HEPB)和催眠性γ-丁内酯(GBL)的结构组合,继承了这两种特性。为了阐明其作用机理,研究了EFBL,GBL和HEPB对多巴胺(DA)和去甲肾上腺素(NA)脑水平的影响。还研究了氯丙嗪,苯乙嗪和氨基氧乙酸的影响。 EFBL以剂量依赖性方式增加DA,在治疗后1小时内在24小时内保持80%的升高,而NA增加54%。第一个小时后,HEPB使DA和NA升高约2倍。分别在3和24小时后,GBL提高了DA和NA。 EFBL逆转了氯丙嗪的作用,但增强了苯乙嗪对DA的作用。氨基氧乙酸既不会改变DA的水平,也不会改变NA的水平,即使在存在EFBL的情况下也是如此。 EFBL的抗惊厥和催眠特性归因于其对突触前多巴胺能受体的作用以及对阻碍其降解的乙基和苯基自由基的持久作用。结果支持DA和NA在调节脑部癫痫发作活动中的作用,并表明EFBL为难治性癫痫提供了一种潜在的治疗方法,无需补充药物和帕金森氏病,而且没有口服疗法的缺点。

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