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  • DC Chemicals Limited
  • China
  • Product Name: Radiprodil
  • Price: $400.0/100mg $750.0/250mg $1300.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

496054-87-6

496054-87-6 structure
496054-87-6 structure
  • Name: Radiprodil
  • Chemical Name: 2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]-2-oxo-N-(2-oxo-3H-1,3-benzoxazol-6-yl)acetamide
  • CAS Number: 496054-87-6
  • Molecular Formula: C21H20FN3O4
  • Molecular Weight: 397.40
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
  • Create Date: 2017-09-13 22:40:48
  • Modify Date: 2024-01-10 17:01:37
  • 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].

Name 2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]-2-oxo-N-(2-oxo-3H-1,3-benzoxazol-6-yl)acetamide
Synonyms UNII-5XGC17ZKUF
Radiprodil
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
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.

Molecular Formula C21H20FN3O4
Molecular Weight 397.40
Exact Mass 397.14400
PSA 95.67000
LogP 3.10320
Storage condition 2-8℃