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GSK1014802 (CNV1014802) is a novel sodium channel blocker [1][2][3].

Voltage-gated sodium channels (Navs) are transmembrane ion channel proteins, which are involved in Na+ ion conduction across cell membranes during cell membrane depolarization [2].

GSK1014802 (CNV1014802) 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. GSK2 inhibited rat forebrain MAO-B with pKi value of 7.20 [1]. CNV1014802 inhibited sodium channels in a state-dependent way. CNV1014802 exhibited selectivity for the Nav1.7 subtype over the other subtypes (Nav1.1, Nav1.2, Nav1.3, Nav1.5, Nav1.6 and TTX-R) [2].

GSK1014802 had completed Phase II trials for lumbosacral radiculopathy and was in phase II trials for trigeminal neuralgia (TN). Furthermore, CNV1014802 was granted orphan drug designation in 2013 by FDA for the treatment of trigeminal neuralgia [3].

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