两种γ-氨基丁酸（GABA）类似物：β-氯GABA和β-苯基GABA的体内和体外生物学作用
Biological actions in vivo and in vitro of two gamma-aminobutyric acid (GABA) analogues: beta-chloro GABA and beta-phenyl GABA.
作者信息
Buu N T, Van Gelder N M
出版信息
Br J Pharmacol. 1974 Nov;52(3):401-6. doi: 10.1111/j.1476-5381.1974.tb08609.x.
1 The synthesis of two analogues of gamma-aminobutyric acid (GABA), beta-chloro GABA and beta-phenyl GABA is described.2 The activity of brain GABA aminotransferase was inhibited by beta-chloro GABA (5.7 x 10(-5)M) and beta-phenyl GABA (4.6 x 10(-3)M) in a competitive manner with GABA.3 beta-Chloro GABA exhibited 50% of the inhibitory activity of GABA in blocking the discharge of the crayfish stretch receptor neurone; beta-phenyl GABA had no detectable effect.4 Injection of beta-phenyl GABA (200 mg/kg) into normal or epileptic cats (cobalt) caused the appearance of synchronized slow-wave EEG activity.5 Administration of beta-chloro GABA (200 mg/kg) to epileptic cats (cobalt) produced a temporary diminution or abolition of epileptic discharges while causing no alteration in normal EEG activity.6 beta-Chloro GABA and beta-phenyl GABA had no effect on the concentrations of catecholamines or of amino acids in mouse brain.7 The results suggest that both beta-chloro GABA and beta-phenyl GABA may pass the blood-brain barrier.
本文描述了γ-氨基丁酸（GABA）的两种类似物β-氯GABA和β-苯基GABA的合成。
β-氯GABA（5.7×10⁻⁵M）和β-苯基GABA（4.6×10⁻³M）以与GABA竞争的方式抑制脑GABA转氨酶的活性。
β-氯GABA在阻断小龙虾牵张感受器神经元放电方面表现出GABA抑制活性的50%；β-苯基GABA没有可检测到的作用。
向正常或癫痫猫（钴致痫）注射β-苯基GABA（200mg/kg）会导致同步慢波脑电图活动的出现。
给癫痫猫（钴致痫）施用β-氯GABA（200mg/kg）会使癫痫放电暂时减少或消失，同时正常脑电图活动无改变。
β-氯GABA和β-苯基GABA对小鼠脑中儿茶酚胺或氨基酸的浓度没有影响。
结果表明，β-氯GABA和β-苯基GABA都可能通过血脑屏障。
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