Löscher W
Arch Int Pharmacodyn Ther. 1980 Jan;243(1):48-55.
Fourteen anticonvulsant drugs were examined for their effects on the activity of GABA-alpha-oxoglutarate aminotransferase (GABA-T). Only the nonspecific enzyme inhibitor aminooxyacetic acid (IC50 2.7 microM) proved to be as potent as the catalytic inhibitors gabaculine (1.8 microM), gamma-acetylenic GABA (150 microM) and gamma-vinyl GABA (350 microM) with respect to inhibition of GABA-T. 2-Methyl-2-ethyl caproic acid, ethanolamine O-sulphate and isoniazid were less effective inhibitors of the GABA-T activity (IC50 greater than 1 mM). None of the clinically established antiepileptic drugs tested (viz. phenobarbital, phenytoin, diazepam, valproate, trimethadione, dimethadione and ethosuximide) produced inhibition comparable to the aforementioned drugs. A slight inhibition of GABA-T (8 to 28%) was seen only with high concentrations of trimethadione, valproate and ethosuximide.
检测了14种抗惊厥药物对γ-氨基丁酸-α-酮戊二酸转氨酶（GABA-T）活性的影响。就抑制GABA-T而言，只有非特异性酶抑制剂氨氧乙酸（IC50为2.7微摩尔）与催化抑制剂加巴脲（1.8微摩尔）、γ-乙炔基-GABA（150微摩尔）和γ-乙烯基-GABA（350微摩尔）一样有效。2-甲基-2-乙基己酸、乙醇胺O-硫酸盐和异烟肼对GABA-T活性的抑制作用较弱（IC50大于1毫摩尔）。所测试的临床常用抗癫痫药物（即苯巴比妥、苯妥英、地西泮、丙戊酸盐、三甲双酮、二甲双酮和乙琥胺）均未产生与上述药物相当的抑制作用。仅在高浓度的三甲双酮、丙戊酸盐和乙琥胺作用下，才观察到对GABA-T有轻微抑制（8%至28%）。
