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Radiprodil

  Cat. No.:  DC12701   Featured
Chemical Structure
496054-87-6
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More than 5000 active chemicals with high quality for research!
Field of application
Radiprodil is an orally active and selective NMDA NR2B antagonist; a potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 496054-87-6
Synonyms: RGH 896,RGH 896,RGH896
SMILES: C1CN(CCC1CC2=CC=C(C=C2)F)C(=O)C(=O)NC3=CC4=C(C=C3)NC(=O)O4
Formula: C21H20FN3O4
M.Wt: 397.4
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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].
Target: NMDA NR2B[1].
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].
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].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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