Sodium Channels

Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.

Raxatrigine (GSK1014802) is a novel sodium channel blocker and is an effective anticonvulsant agent. In rats, GSK1014802 (20 - 80 mg/kg p.o.) attenuated the deficit in reversal learning induced by phencyclidine (PCP) in a dose-dependent way, which suggested the potential of GSK1014802 in the treatment of cognitive symptoms of schizophrenia. GSK2 was also a potent inhibitor of human MAO-B with pIC50 value of 7.96 but did not inhibit human MAO-A.

Encainide HCl is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative.

Disopyramide is an antiarrhythmic (class IA) and a sodium channel blocker.

ENIPORIDE is a potent Na+/H+ exchange inhibitor.

beta-Pompilidotoxin is a peptide with the sequence H2N-Arg.

Pilsicainide is a water soluble selective Na+ channel blocker.

PF-05089771 is a Selective Nav1.7 Inhibitor (IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV.

PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.

XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits hNaV1.7 with IC50 of 3 nM.

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