Schechter P J, Tranier Y
Psychopharmacology (Berl). 1977 Oct 20;54(2):145-8. doi: 10.1007/BF00426770.
gamma-Acetylenic GABA and gamma-vinyl GABA, two catalytic irreversible inhibitors of mammalian brain GABA transaminase that produce several-fold increases in brain GABA concentrations were tested for their effects on bicuculline and picrotoxin-induced seizures and mortality in mice. Neither inhibitor influenced the frequency of seizures or death produced by either bicuculline or picrotoxin. Both inhibitors, however, produced a dose-dependent prolongation of the time to onset of seizures and death induced by picrotoxin but by bicuculline. These results suggest differences in the antagonism by bicuculline and picrotoxin of GABA-mediated neural functions.
γ-乙炔基 GABA 和 γ-乙烯基 GABA 是哺乳动物脑 GABA 转氨酶的两种催化性不可逆抑制剂，它们可使脑内 GABA 浓度增加数倍。研究测试了这两种抑制剂对荷包牡丹碱和印防己毒素诱发小鼠癫痫发作及致死率的影响。两种抑制剂均未影响荷包牡丹碱或印防己毒素诱发的癫痫发作频率或死亡率。然而，两种抑制剂均使印防己毒素而非荷包牡丹碱诱发的癫痫发作和死亡的发作时间出现剂量依赖性延长。这些结果表明，荷包牡丹碱和印防己毒素对 GABA 介导的神经功能的拮抗作用存在差异。
