Battistin L, Varotto M, Berlese G, Roman G
Neurochem Res. 1984 Feb;9(2):225-31. doi: 10.1007/BF00964170.
The effect of anticonvulsant drugs was examined on brain GABA levels and GAD and GABA-T activities. The level of GABA was increased by the treatment with diphenylhydantoin. The drug had no effect on GABA-T activity, whereas GAD activity was inhibited. Carbamazepine increased the GABA level but did not effect GAD and GABA-T activities. Diazepam had no effect on GABA level and GAD activity, whereas it caused a slight inhibition of GABA-T activity. Phenobarbital administration decreased GABA level only at the higher concentration. Clonazepam effected only GAD activity. Some anticonvulsant drugs generally increase brain GABA level; however the lack of correlation with an effect on the GAD and GABA-T activities indicate that other factors than metabolism, such as membrane transport processes, are involved in the mechanism of action of anticonvulsant drugs.
研究了抗惊厥药物对脑内γ-氨基丁酸(GABA)水平、谷氨酸脱羧酶(GAD)和GABA转氨酶(GABA-T)活性的影响。用苯妥英治疗可使GABA水平升高。该药物对GABA-T活性无影响,而GAD活性受到抑制。卡马西平可提高GABA水平,但对GAD和GABA-T活性无影响。地西泮对GABA水平和GAD活性无影响,而对GABA-T活性有轻微抑制作用。仅在较高浓度时,苯巴比妥给药会降低GABA水平。氯硝西泮仅影响GAD活性。一些抗惊厥药物通常会提高脑内GABA水平;然而,与对GAD和GABA-T活性的影响缺乏相关性表明,除代谢外的其他因素,如膜转运过程,参与了抗惊厥药物的作用机制。