riluzole

Riluzole (RP-54274) 是一种谷氨酸拮抗剂，用作抗惊厥药并延长肌萎缩侧索硬化症患者的生存期。它还抑制 GABA 摄取，IC50值为 43 μM。

Riluzole-13C,15N2 is intended for use as an internal standard for the quantification of riluzole by GC- or LC-MS. Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED50 value of 3.2 mg kg and displays neuroprotective effects in hypoxic animals at an ED50 value of 4 mg kg. Formulations containing riluzole have been explored as therapeutics for slowing disease progression of amyotrophic lateral sclerosis.

N-hydroxy Riluzole is a metabolite of the antiglutamatergic agent riluzole .1It is formed from riluzole predominantly by the cytochrome P450 (CYP) isoform CYP1A2 in human hepatic microsomes. 1.Sanderink, G.J., Bournique, B., Stevens, J., et al.Involvement of human CYP1A isoenzymes in the metabolism and drug interactions of riluzole in vitroJ. Pharmacol. Exp. Ther.282(3)1465-1472(1997)

Riluzole hydrochloride (PK 26124 hydrochloride) 是一种抗惊厥化合物，属于钠通道阻滞剂家族，抑制 GABA 摄取。Riluzole hydrochloride是钠-谷氨酸拮抗剂，具有抗癌和神经保护活性，可用于研究肌萎缩侧索硬化症和神经系统疾病。

VGSCs-IN-1 是一种有效的 VGSC 抑制剂，是一种 Riluzole 的 2-哌嗪类似物，在Nav1.4上展现出良好的阻断活性。VGSCs-IN-1可用于研究细胞兴奋性障碍。

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) 。