氨己烯酸和噻加宾单独及联合应用于小鼠皮层的神经化学作用

Neurochemical actions of vigabatrin and tiagabine alone and in combination in mouse cortex.

Leach J P, Sills G J, Butler E, Forrest G, Thompson G G, Brodie M J

University Department of Medicine and Therapeutics, Western Infirmary, Glasgow, Scotland.

Gen Pharmacol. 1997 May;28(5):715-9. doi: 10.1016/s0306-3623(96)00357-6.

Abstract

The effects of repeated administration of the anticonvulsant compounds, vigabatrin (VGB) and tiagabine (TGB), on gamma-aminobutyric acid (GABA) concentration and the activities of GABA-transaminase (GABA-T) and glutamic acid decarboxylase (GAD) were investigated in mouse cortex. 2. VGB alone increased GABA levels and decreased GABA-T and GAD activities. 3. TGB alone was essentially without effect. 4. Low doses of VGB and TGB in combination increased GABA levels when neither drug had such an effect alone. 5. Despite this observation, this study failed to establish any conclusive evidence for an interaction between VGB and TGB that might help to explain their reported clinical synergism.

摘要

研究了抗惊厥化合物氨己烯酸（VGB）和噻加宾（TGB）重复给药对小鼠皮层中γ-氨基丁酸（GABA）浓度以及GABA转氨酶（GABA-T）和谷氨酸脱羧酶（GAD）活性的影响。2. 单独使用VGB可提高GABA水平，并降低GABA-T和GAD活性。3. 单独使用TGB基本无作用。4. 当两种药物单独使用均无此作用时，低剂量的VGB和TGB联合使用可提高GABA水平。5. 尽管有此观察结果，但本研究未能找到任何确凿证据证明VGB和TGB之间存在相互作用，而这种相互作用可能有助于解释它们所报道的临床协同作用。