glutamate transporter 1

LDN-212320 (OSU-0212320) 是兴奋性氨基酸转运体 2(EAAT2) 谷氨酸转运体(GLT-1)的激活剂。它通过上调海马和 ACC 星形胶质细胞 GLT-1 的水平来预防伤害性疼痛。

EAAT2 activator 1 (3-[(2-Chloro-6-fluorobenzyl)thio]-6-pyridin-2-ylpyridazine) 是兴奋性氨基酸转运蛋白 2(EAAT2) 的有效激活剂，以剂量依赖性方式增加 EAAT2 蛋白水平。

GPI-1046 是一种无抗生素作用的亲免素配体，部分通过上调 PFC 和 NAc 核心中的谷氨酸转运蛋白 1 来减少乙醇摄入。

Erastin2 是一种铁死亡诱导剂，通过与亲脂性自由基捕获抗氧化剂ferrostatin-1或铁螯合剂去铁胺（DFO）来诱导细胞死亡。

DL-TBOA ammonium is a potent, non-transportable inhibitor of excitatory amino acid transporters. Its inhibitory effects are demonstrated by IC50 values of 70 μM, 6 μM, and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2, and EAAT3, respectively. Additionally, DL-TBOA ammonium significantly hampers the uptake of [14C]glutamate in COS-1 cell lines expressing human EAAT1 and EAAT2, evident by Ki values of 42 μM and 5.7 μM, respectively. Furthermore, this compound competitively blocks EAAT4 and EAAT5, with Ki values of 4.4 μM and 3.2 μM, respectively.