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长期给予γ-氨基丁酸转氨酶抑制剂后大鼠脑内的微空泡形成。乙醇胺-O-硫酸盐和氨己烯酸作用的比较。

Micro-vacuolation in rat brains after long term administration of GABA-transaminase inhibitors. Comparison of effects of ethanolamine-O-sulphate and vigabatrin.

作者信息

John R A, Rimmer E M, Williams J, Cole G, Fowler L J, Richens A

出版信息

Biochem Pharmacol. 1987 May 1;36(9):1467-73. doi: 10.1016/0006-2952(87)90112-2.

DOI:10.1016/0006-2952(87)90112-2
PMID:3579985
Abstract

Two "suicide" inhibitors of GABA-aminotransferase which are known to raise the concentration of GABA in vivo and to have anti-convulsant properties, have been compared for the extent to which they produce micro-vacuoles in the brains of rats. The compounds gamma-vinyl-GABA (Vigabatrin) and ethanolamine-O-sulphate were administered orally for six months to rats at doses that produced the same increase in brain GABA levels. Micro-vacuolation was found to be present in the brains of animals treated with either compound but to be more severe in those treated with Vigabatrin. A quantitative assessment using computerised image analysis revealed that both the number of vacuoles, and the area occupied by them, was twice as high in the Vigabatrin treated animals as in those treated with ethanolamine-O-sulphate. This quantitative difference could be seen to be due to the fact that in the Vigabatrin treated animals the vacuoles extended into the white matter tracts between the cerebellar folia whereas in those animals treated with ethanolamine-O-sulphate it was confined to the roof nucleus.

摘要

已知两种γ-氨基丁酸转氨酶的“自杀性”抑制剂可在体内提高γ-氨基丁酸(GABA)的浓度并具有抗惊厥特性,本文对它们在大鼠脑中产生微空泡的程度进行了比较。将化合物γ-乙烯基-GABA(vigabatrin)和乙醇胺-O-硫酸盐以能使脑GABA水平产生相同升高的剂量口服给予大鼠六个月。发现用任一化合物处理的动物脑中均存在微空泡形成,但在用vigabatrin处理的动物中更严重。使用计算机图像分析进行的定量评估显示,vigabatrin处理的动物中的空泡数量及其所占面积是乙醇胺-O-硫酸盐处理动物的两倍。这种定量差异可能是由于在vigabatrin处理的动物中,空泡延伸至小脑叶片之间的白质束,而在用乙醇胺-O-硫酸盐处理的动物中,空泡局限于顶核。

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