首页> 外文期刊>Japanese Journal of Pharmacology >Effect of NC-1100 [1-(3, 4-Dimethoxyphenyl)-2-(4-Diphenylmethylpiperazinyl) Ethanol Dihydrochloride] on γ-Aminobutyric Acid (GABA) Metabolism in Rat Brain: Analysis Using Stroke-Prone Spontaneously Hypertensive Rat
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Effect of NC-1100 [1-(3, 4-Dimethoxyphenyl)-2-(4-Diphenylmethylpiperazinyl) Ethanol Dihydrochloride] on γ-Aminobutyric Acid (GABA) Metabolism in Rat Brain: Analysis Using Stroke-Prone Spontaneously Hypertensive Rat

机译:NC-1100 [1-(3,4-二甲氧基苯基)-2-(4-二苯基甲基哌嗪基)乙醇二盐酸盐]对大鼠脑中γ-氨基丁酸(GABA)代谢的影响:使用中风自发性高血压大鼠的分析

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References(16) Cited-By(2) Effects of oral administration of NC-1100 on the metabolism of neuroactive amino acids in rat brain were studied using stroke-prone spontaneously hypertensive (SHR-SP) and Wistar Kyoto rats. The repeated administration of NC-1100 induced a significant increase of γ-aminobutyric acid (GABA) content in the cerebellum and medulla oblongata of SHR-SP. The decrease of aspartic acid contents in the cerebellum and medulla oblongata of SHR-SP was also noted following NC-1100 administration. Although the activity of L-glutamic acid decarboxylase did not change in these cerebral areas, the activity of GABA-transaminase:succinic semialdehyde dehydrogenase was found to be significantly reduced in the cerebellum of SHR-SP following the repeated administration of NC-1100. The turnover rate of GABA was also significantly reduced in the cerebellum and medulla oblongata of SHR-SP. It was also found that the spontaneous release of preloaded [3H]GABA from cerebral cortical slices was significantly retarded by the continuous oral administration of NC-1100. These results suggest that NC-1100 may be a drug inducing the increase of GABA in the cerebellum and medulla oblongata following continuous administration, especially in animals having hypertension associated cerebrovascular disorders such as SHR-SP.
机译:参考文献(16)(2)使用中风倾向性自发性高血压(SHR-SP)和Wistar Kyoto大鼠研究了NC-1100口服对大鼠脑中神经活性氨基酸代谢的影响。重复施用NC-1100会导致SHR-SP的小脑和延髓中γ-氨基丁酸(GABA)含量显着增加。在NC-1100给药后,还注意到SHR-SP的小脑和延髓中天冬氨酸含量的降低。尽管在这些脑区中L-谷氨酸脱羧酶的活性没有改变,但是在重复施用NC-1100后,发现SHR-SP小脑中的GABA-转氨酶:琥珀酸半醛脱氢酶的活性显着降低。 SHR-SP的小脑和延髓中GABA的转换率也显着降低。还发现,通过连续口服NC-1100,预加载的[3H] GABA自大脑皮层片的自发释放明显受到阻碍。这些结果表明,NC-1100可能是一种在连续给药后引起小脑和延髓中GABA增加的药物,特别是在患有高血压相关性脑血管疾病如SHR-SP的动物中。

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