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Radiprodil

CAS No. : 496054-87-6

MCE 站：Radiprodil

产品活性：Radiprodil (RGH-896) 是具有口服活性的、NMDA 受体 NR2B 亚类的选择性拮抗剂。是一种可用于治疗神经性疼痛和其它慢性疼痛的潜在药物。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：iGluR

In Vitro: Preincubation with Radiprodil (10 nM) restores long-term potentiation (LTP) in the presence of Aβ_1-42, 3NTyr10-Aβ and Aβ_1-40, but not AβpE3.
As for LTP, Radiprodil (10 nM) reverses the synaptic toxicity of 3NTyr-AβAβ_1-40 and Aβ_1-42 but not that AβpE_3-42.

In Vivo: Radiprodil could block NMDA currents in Mg²⁺ insensitive variants, with potencies similar to those obtained without Mg²⁺.
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.

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