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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
CNV 1014802 (also known as Vixotrigine, Raxatrigine) is a state-dependent voltage-gated sodium channel blocker with anticonvulsant and analgesic pharmacology.
Voltage-gated sodium channels regulate neuronal excitability and pain transmission, with Nav1.7 and related channels playing important roles in sensory neuron firing. CNV 1014802 is used to study sodium-channel blockade in neuropathic pain and CNS excitability models.
Key Features
- Voltage-gated sodium channel blocker
- Also known as raxatrigine, vixotrigine and BIIB074
- Relevant to Nav-mediated pain and excitability pathways
- Clinically investigated for neuropathic pain and trigeminal neuralgia
Applications
- Sodium channel pharmacology
- Neuropathic pain and trigeminal neuralgia models
- Sensory neuron excitability assays
- Electrophysiology and anticonvulsant mechanism studies
Note: The water soluble salt, CNV1014802 hydrochloride (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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