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CNV1014802 (hydrochloride)

Names

[ CAS No. ]:
934240-31-0

[ Name ]:
CNV1014802 (hydrochloride)

[Synonym ]:
(5R)-(4-{[(2-fluorophenyl)methyl]oxy}phenyl)-L-prolinamide hydrochloride
(5R)-5-(4-[2-fluorobenzyloxy]phenyl)-L-prolinamide hydrochloride
CNV1014802 (hydrochloride)
GSK-1014802
Raxatrigine hydrochloride

Biological Activity

[Description]:

CNV1014802(GSK-1014802) Hcl is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.IC50 value: Target: sodium channel blockerLike 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. CNV1014802 received orphan-drug designation from the US Food and Drug Administration in July 2013.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel
Research Areas >> Neurological Disease

[References]

[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.


[Related Small Molecules]

EIPA | Riluzole | Ginsenoside Rg3 | Cariporide | Eleclazine hydrochloride | GS967 | Tenapanor | Triamterene | Ranolazine dihydrochloride | PF 05089771 | flecainide acetate | A-803467 | Zonisamide | Cinchocaine | ICA 121431

Chemical & Physical Properties

[ Molecular Formula ]:
C18H20ClFN2O2

[ Molecular Weight ]:
350.81500

[ Exact Mass ]:
350.12000

[ PSA ]:
64.35000

[ LogP ]:
4.51420


Related Compounds