Lu AE98134, an activator of voltage-gated sodium channels , acts as a partly selective Na v 1.1 channels positive modulator. Lu AE98134 also increases the activity of Na v 1.2 and Na v 1.5 channels but not of Na v 1.4, Na v 1.6 and Na v 1.7 channels. Lu A
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Product Description
Lu AE98134, an activator of voltage-gated sodium channels , acts as a partly selective Na v 1.1 channels positive modulator. Lu AE98134 also increases the activity of Na v 1.2 and Na v 1.5 channels but not of Na v 1.4, Na v 1.6 and Na v 1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Na v 1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al.
In Vitro
Lu AE98134 (30 μM) promotes the current mediated by Nav v 1.1 channel, and it activates Na v 1.5 and to a lesser extent Na v 1.2 but has no effect on Na v 1.4, Na v 1.6 and Na v 1.7 currents in HEK cells expressing Na v 1.1, Na v 1.2, Na v 1.6, Na v 1.5, and Na v 1.7 by step-wise depolarizing voltages using the whole-cell patchclamp configuration. Lu AE98134 (30 μM) increases the excitability of FSINs by decreasing the threshold for action potentials.Intracellular depolarizing current pulses evokes repetitive firing of action potentials at frequencies, additionally, Lu AE98134 increases the excitability since each current pulse generated a higher number of spikes (163 spikes in control; and 230 spikes in Lu AE98134). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The fast spiking inhibitory interneurons (FSINs) from Dlx5/6 +/− animals exhibit abnormal excitability because of a more depolarized spike threshold and broader action potentials. Lu AE98134 (30 μM) increases the excitability of FSINs neurons from normal and Dlx5/6 +/− animals by modulating several parameters characteristic for NaV 1.1 channels. The selective activation of FSINs by Lu AE98134 restores cognitive flexibility in adult Dlx5/6 +/− mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
