glutamate uptake

Cis-ACBD (cis-1-aminocyclobutane-1,3-dicarboxylic acid) 是一种有效的选择性 N-甲基-D-天冬氨酸受体激动剂。

Evans blue (C.I. 23860) 是一种突触泡谷氨酸吸收的有效抑制剂，同时也是一种AMPA kainate 受体拮抗剂。

Zonisamide (AD 810) 是锌酶碳酸酐酶 (carbonic anhydrase) 的有效抑制剂，对人类线粒体同工酶 hCA II 和 hCA V 作用的 Ki 值分别为 35.2 nM 和 20.6 nM。Zonisamide 具有抗癫痫活性，在癫痫、癫痫发作和帕金森病的研究中具有价值。

Afoxolaner 是一种异恶唑啉杀虫剂 杀螨剂，可对抗犬的肩胛硬蜱。 它作用于昆虫的 γ-氨基丁酸(GABA)受体谷氨酸受体，抑制 GABA 和谷氨酸调节的氯离子吸收，导致过度的神经元刺激和节肢动物死亡。

BCATc Inhibitor 2 是选择性分支链氨基转移酶抑制剂，可用于神经退行性疾病的研究。能够抑制 rBCATc (IC50:0.2 μM)，hBCATc (IC50:0.8 μM)、 rBCATm (IC50:3.0 μM)。其中BCATc 也称为 BCAT1，存在于细胞质基质中的亚型。

EAAT2(GLT1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake

inhibitor of both glial and neuronal uptake of glutamate, aspartate and cysteate.

WAY-855 is an EAAT2-preferring, nonsubstrate inhibitor of high-affinity glutamate uptake.

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.

Nε-(1-Carboxyethyl)-L-lysine (CEL), a known advanced glycation end product (AGE), forms through the interaction of methyl glyoxal and lysine residues within proteins. Unlike its free form, protein-bound CEL can attach to the receptor for AGEs (RAGE). Its concentrations are notably higher in the lenses of diabetic cataract patients and are reduced in rat heart mitochondria following sustained caloric restriction. Furthermore, at 1 mM, CEL impedes glutamate uptake and the release of S100B in rat hippocampal slices, an effect that occurs independently of RAGE.

Zonisamide-d4 是 Zonisamide 的氘代化合物。Zonisamide 的 CAS 号为 68291-97-4。Zonisamide 是锌酶碳酸酐酶 (carbonic anhydrase) 的有效抑制剂，对人类线粒体同工酶 hCA II 和 hCA V 作用的Ki值分别为 35.2 nM 和 20.6 nM。Zonisamide 具有抗癫痫活性，在癫痫、癫痫发作和帕金森病的研究中具有价值。

Troriluzole hydrochloride 是 Riluzole 的第三代三肽前体，是一种口服活性的谷氨酸调节剂。它能够降低突触谷氨酸水平，并提高突触谷氨酸的吸收效率。Troriluzole hydrochloride 展现出治疗阿尔茨海默病和广泛性焦虑症 (GAD) 的潜在应用。