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CNV 1014802
- GSK 1014802 - GSK2 - Raxatrigine - BIIB 074,Vixotrigine
- Optical Purity: Optically pure
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C18H19FN2O2
- MW: 314.35
Description
Sodium channel blocker with potent anticonvulsant activity; potential for novel treatment for Schizophrenia. CNV 1014802 (GSK 1014802 or GSK2 or Raxatrigine) was tested in clinical trials for treatment of trigeminal neuralgia, and shows selectivity for the Nav1.7 subtype over the other subtypes tested (Nav1.1, Nav1.2, Nav1.3, Nav1.5, Nav1.6 and TTX-R), for both the resting and depolarized states.
The water soluble HCl salt of CNV 1014802 (Axon 2548) is available as well
More Information
| Parent CAS No. | 934240-30-9 |
|---|---|
| Chemical Name | (2S,5R)-5-(4-(2-fluorobenzyloxy)phenyl)pyrrolidine-2-carboxamide |
| SMILES | N1[C@@H](C2=CC=C(OCC3=CC=CC=C3F)C=C2)CC[C@H]1C(N)=O |&1:1,19,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C18H19FN2O2/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)/t16-,17+/m1/s1 |
| InChiKey | JESCETIFNOFKEU-SJORKVTESA-N |
| CID | 16046068 |
| Short Description | Na+ channel blocker |
References
- CH Large 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, 338(1), 100-113.
- J.M. Zakrzewska et al. Novel design for a phase IIa placebo-controlled, double-blind randomized withdrawal study to evaluate the safety and efficacy of CNV1014802 in patients ith trigeminal neuralgia. Trials. 2013 Nov 23;14:402.
- A. Nardi et al. Advances in targeting voltage-gated sodium channels with small molecules. ChemMedChem. 2012 Oct;7(10):1712-40.
- C.H. Large et al. The relationship between sodium channel inhibition and anticonvulsant activity in a model of generalised seizure in the rat. Epilepsy Res. 2009 Jul;85(1):96-106.
- JR Deuis et al. Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain. Toxins (Basel). 2016 Mar 17;8(3). pii: E78.
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