Gram L
University Clinic of Neurology, Hvidovre Hospital, Denmark.
Epilepsia. 1994;35 Suppl 5:S85-7. doi: 10.1111/j.1528-1157.1994.tb05977.x.
The various possibilities for manipulating the gamma-aminobutyric acid (GABA) system to augment GABAergic inhibition have been surveyed with reference to the relevant antiepileptic compounds that have been successfully or unsuccessfully investigated in relation to these different mechanisms of action. The first clinical studies of tiagabine (TGB), a novel GABA-uptake inhibitor are now available. These studies utilized a novel design, the enrichment (Amery) design, which is put into perspective compared to classical clinical trial designs. Possible advantages and disadvantages of TGB, as seen at this stage in development, have been identified.
针对已成功或未成功研究的与这些不同作用机制相关的抗癫痫化合物，探讨了操纵γ-氨基丁酸（GABA）系统以增强GABA能抑制作用的各种可能性。新型GABA摄取抑制剂替加宾（TGB）的首批临床研究现已可得。这些研究采用了一种新型设计，即富集（阿梅里）设计，并与经典临床试验设计进行了对比分析。已确定了TGB在现阶段开发中可能存在的优缺点。
