Department of Pharmacy, Center for Drug Research, Ludwig-Maximilians-University Munich, Butenandtstr. 5-13, D-81377 Munich, Germany.
Eur J Med Chem. 2011 May;46(5):1483-98. doi: 10.1016/j.ejmech.2011.01.042. Epub 2011 Feb 3.
A new series of potential GABA uptake inhibitors starting from of 1H-imidazol-4-ylacetic acid with the carboxylic acid side chain originating from different positions and varying in length have been synthesized and tested for the inhibitory potency at the four GABA uptake transporters mGAT1-4 stably expressed in HEK cells. Further two bicyclic compounds with a rigidified carboxylic acid side chain were included in this study. The results of the biological tests indicated that most ω-imidazole alkanoic and alkenoic acid derivatives exhibit the highest potencies as GABA uptake inhibitors at mGAT3.
已合成并测试了一系列以 1H-咪唑-4-乙酸为起始物的新型潜在 GABA 摄取抑制剂，其羧酸侧链源自不同位置且长度不同，用于抑制在稳定表达于 HEK 细胞的四种 GABA 摄取转运体 mGAT1-4 上的抑制效力。本研究还包括两个具有刚性羧酸侧链的双环化合物。生物测试结果表明，大多数 ω-咪唑烷烷酸和烯酸衍生物在 mGAT3 上作为 GABA 摄取抑制剂表现出最高的效力。
