Radiprodil

Names

[ Name ]:
Radiprodil

[Synonym ]:
UNII-5XGC17ZKUF
Radiprodil

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[Target]

NMDA NR2B[1].

[In Vitro]

Preincubation with Radiprodil (10 nM) restores long-term potentiation (LTP) in the presence of Aβ1-42, 3NTyr10-Aβ and Aβ1-40, but not AβpE3[2]. As for LTP, Radiprodil (10 nM) reverses the synaptic toxicity of 3NTyr-AβAβ1-40 and Aβ1-42 but not that AβpE3-42[2].

[In Vivo]

Radiprodil could block NMDA currents in Mg2+ insensitive variants, with potencies similar to those obtained without Mg2+[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].

[References]

[1]. Mony L, et al. Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential. Br J Pharmacol. 2009 Aug;157(8):1301-17.

[2]. Rammes G, et al. The NMDA receptor antagonist Radiprodil reverses the synaptotoxic effects of different amyloid-beta (Aβ) species on long-term potentiation (LTP). Neuropharmacology. 2018 Sep 15;140:184-192.

[3]. Mullier B, et al. GRIN2B gain of function mutations are sensitive to radiprodil, a negative allosteric modulator of GluN2B-containing NMDA receptors. Neuropharmacology. 2017 Sep 1;123:322-331.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₂₀FN₃O₄

[ Molecular Weight ]:
397.40

[ Exact Mass ]:
397.14400

[ PSA ]:
95.67000

[ LogP ]:
3.10320

[ Storage condition ]:
2-8℃