化合物Radiprodil T5385

Product Introduction
Bioactivity


英文名: Radiprodil

描述: Radiprodil (RGH-896) 是一种具有口服活性的、NMDA 受体 NR2B 亚类的选择性拮抗剂。它有用于神经性疼痛和其它慢性疼痛的相关研究潜力。

体外活性: The inhibition potency of ligands toward the NR2B NMDA receptors was evaluated by measuring the Ca2t influx evocated by NMDA application (at 100 mM for 30 s) in NR1a/NR2B subunit transfected HEK cells. Radiprodil had potent inhibitory effects (69 nM) towards Ca2+ influx [1]. A low concentration (10?nM) of the GLUN2B receptor antagonist Radiprodil restored LTP in the presence of Aβ1-42, 3NTyr10-Aβ, Aβ1-40, but not AβpE3. Radiprodil (10?nM) reversed the synaptic toxicity of Aβ species but not that of AβpE3 [2].

体内活性: Radiprodil 在小鼠甲醛试验中的体内镇痛效能为 7.7 mg/kg p.o. (ED50)，目前正在进行一项与 Radiprodil [1] 相关的临床试验。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 220 mg/mL (553.6 mM)


关键字: Ionotropic glutamate receptors | RGH896 | iGluR | inhibit | Radiprodil | Inhibitor | RGH 896

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途