Nav1.1activator1(compound4)是强有效的、能透过血脑屏障的、Nav1.1激动剂，0.03μM可增加衰减Nav1.1电流的时间常数τ。对Nav1.2、Nav1.5、Nav1.6有显著的选择性。
Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6[1].
Nav1.1 activator 1 (compound 4) is a valuable Nav1.1 activator for further evaluation of pathophysiological functions of the Nav1.1 channel and has potential for therapeutic treatments of CNS diseases such as Dravet syndrome[1]. Animal Model: Mice[1].
[1]. Miyazaki T, et al. Discovery of novel 4-phenyl-2-(pyrrolidinyl)nicotinamide derivatives as potent Nav1.1 activators. Bioorg Med Chem Lett. 2019 Mar 15;29(6):815-820.
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