Raxatrigine hydrochloride (GSK-1014802 hydrochloride) 是钠离子通道Nav1.7有效抑制剂。

Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

Solid

Sodium channel blocker.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : ≥ 31 mg/mL (88.36 mM)H₂O : 14.29 mg/mL (40.73 mM; Need ultrasonic)