glutamate transporters

Chelidamic acid 是一种有效的谷氨酸脱羧酶抑制剂(Ki:33 μM)，也是含有吡喃骨架的杂环有机酸，与金属离子有良好的配位能力。

Troriluzole 是一种具有口服活性谷氨酸调节剂，具有抗癌活性。Troriluzole 可提高位于神经胶质细胞的兴奋性氨基酸转运体的表达，可用于研究脊髓小脑性共济失调、阿尔茨海默病和广泛性焦虑症 (GAD) 。

MS-153, 作为一种激活谷氨酸转运体的化合物, 已经被证明可以减少吗啡、甲基苯丙胺和可卡因的条件性奖赏效应，而不会对小鼠的急性运动反应产生负面影响。

Prasterone is an endogenous steroid hormone. Prasterone acts as an agonist at ERβ, NMDA, and σ1 receptors, a partial agonist at ERα and AR, and antagonist at GABA-A receptors. It displays a variety of biologocial activities, including enhancing working me

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.

(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) 是一种选择性且非竞争性的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂，Ki 为 211.7 nM。它是一种 Dizocilpine 的活性较低的 (-)-对映体，具有抗抑郁作用。

YM 298198 Hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM). YM 298198 Hydrochloride is inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). It inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively).