Radiprodil

496054-87-6

C21H20FN3O4

DMSO : 250 mg/mL (629.09 mM; Need ultrasonic)

Membrane Transporter/Ion Channel; Neuronal Signaling

Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions^[1]. IC50 & Target: NMDA NR2B^[1]. In Vitro: Preincubation with Radiprodil (10 nM) restores long-term potentiation (LTP) in the presence of Abeta_1-42, 3NTyr10-Abeta and Abeta_1-40, but not AbetapE3^[2].
As for LTP, Radiprodil (10 nM) reverses the synaptic toxicity of 3NTyr-AbetaAbeta_1-40 and Abeta_1-42 but not that AbetapE_3-42^[2].
In Vivo: Radiprodil could block NMDA currents in Mg²⁺ insensitive variants, with potencies similar to those obtained without Mg^2+[3].
Radiprodil's potency is higher at pH 7.0 than at pH 7.6, suggesting that radiprodil may retain its ability to block glutamate-induced NMDA currents even under acidic conditions that manifest under long term seizures^[3].