Raxatrigine hydrochloride

• CAT Number: I008981
• CAS Number: 934240-31-0
• Molecular Formula: C18H20ClFN2O2
• Molecular Weight: 350.82
• Purity: ≥95%
• Synonyms: (2S,5R)-5-[4-[(2-fluorophenyl)methoxy]phenyl]pyrrolidine-2-carboxamide;hydrochloride
• InChI: InChI=1S/C18H19FN2O2.ClH/c19-15-4-2-1-3-13(15)11-23-14-7-5-12(6-8-14)16-9-10-17(21-16)18(20)22;/h1-8,16-17,21H,9-11H2,(H2,20,22);1H/t16-,17+;/m1./s1
• InChIKey: HEPUBAGOKRIZEO-PPPUBMIESA-N
• SMILES: C1CC(NC1C2=CC=C(C=C2)OCC3=CC=CC=C3F)C(=O)N.Cl

Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
Like lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus confirming their potential in the treatment of cognitive symptoms of schizophrenia. However, higher doses than those required for anticonvulsant efficacy of the drugs were needed for activity in the reversal-learning model, suggesting a lower therapeutic window relative to mechanism-dependent central side effects for this indication. Raxatrigine (GSK-1014802) received orphan-drug designation from the US Food and Drug Administration in July 2013.

Reference

[1]. Large CH, et al. The efficacy of sodium channel blockers to prevent phencyclidine-induced cognitive dysfunction in the rat: potential for novel treatments for schizophrenia. J Pharmacol Exp Ther. 2011 Jul;338(1):100-13.
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