Radiprodil 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。

Radiprodil (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP).

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].

The in vivo analgesic efficiency for 1a in the mouse formalin test was 7.7 mg/kg p.o. (ED50) and a clinical trial is currently conducted with Radiprodil [1].

496054-87-6

C21H20FN3O4

397.406

RGH-896

DMSO:220 mg/mL (553.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years