Radiprodil is a selective antagonist of NMDA NR2B that used in treatment of neuropathic pain.
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Radiprodil (RGH-896) is an orally active, selective NMDA NR2B antagonist, identified as a potential treatment for neuropathic pain and possibly other chronic pain conditions[1].
体内研究
Radiprodil blocks NMDA currents in Mg2+ insensitive variants with similar potencies to those without Mg2+[3].
Radiprodil demonstrates greater efficacy at pH 7.0 compared to pH 7.6, indicating its potential to sustain blockade of glutamate-induced NMDA currents amidst acidic conditions associated with prolonged seizures [3].
体外研究
Pre-treatment with Radiprodil (10 nM) restores long-term potentiation (LTP) affected by Aβ1-42, 3NTyr10-Aβ, and Aβ1-40, although not by AβpE3[2].
Regarding LTP, Radiprodil (10 nM) counteracts the synaptic toxicity caused by 3NTyr-Aβ, Aβ1-40, and Aβ1-42, but it does not affect the toxicity induced by AβpE3-42[2].
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