354812-16-1

AA43279 (354812-16-1) is a selective Nav1.1 activator. In HEK-293 cells expressing human Nav1.1 channels AA43279 increased the Nav1.1-mediated current in a concentration dependent manner (EC50=9.5 μM). In rat hippocampal brain slices it increased the firing activity of parvalbumin-expressing, fast-spiking GABAergic interneurons and increased the spontaneous inhibitory post-synaptic currents recorded from pyramidal neurons. It displayed anticonvulsant activity in vivo. Important tool compound for exploring the physiology of Nav1.1 channels.1

AA43279 is an in gamma-aminobutyric acid (GABA) fast-firing interneurons located activator for Nav1.1 channel (SCN1A) with an EC50 of 9.5 μM. AA43279 enhances specific neuronal firing activity in vitro, and exhibits anticonvulsant activity in rat MEST model[1].

Nav1.1: 9.5 μM (IC₅₀); Nav1.6: 11.6 μM (IC₅₀); Nav1.5: 14.4 μM (IC₅₀); Nav1.2: 22.8 μM (IC₅₀)

1) Frederiksen et al. (2017), A small molecule activator of Nav 1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo.; Eur. J. Neuroscience, 46 1887