Nav1.1 activator 1 (compound 4) is a highly potent Nav1.1 activator with BBB penetration, which increases the decay time constant (tau) of Nav1.1 currents at 0.03 μM, demonstrating significant selectivity against Nav1.2, Nav1.5, and Nav1.6.
- A valuable Nav1.1 activator for further evaluation of pathophysiological functions of the Nav1.1 channel.
- Has potential for therapeutic treatments of Central Nervous System (CNS) diseases like Dravet syndrome.
- Intraperitoneal administration (30 mg/kg) in mice achieved sufficient brain exposure (193 ng/g 1 hour after administration), corresponding to 13 nM of free brain concentration, comparable to its in vitro potency.
- Capable of penetrating the blood-brain barrier (BBB) in humans.