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Lu AE98134

CAS No. : 849000-18-6

MCE 国际站：Lu AE98134

产品活性：Lu AE98134 是电压门控钠通道 (voltage-gated sodium channels) 的激活剂，作为 Na_v1.1 通道的部分选择性激活剂。Lu AE98134 也可以增加 Na_v1.2 和 Na_v1.5 通道的活性，但对 Na_v1.4、Na_v1.6 和 Na_v1.7 通道活性无明显影响。Lu AE98134 可用于分析 Na_v1.1 通道在各种中枢神经系统疾病中的病理生理功能，如精神分裂症等。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Sodium Channel

In Vitro: Lu AE98134 (30 μM) promotes the current mediated by Nav_v1.1 channel, and it activates Na_v1.5 and to a lesser extent Na_v1.2 but has no effect on Na_v1.4, Na_v1.6 and Na_v1.7 currents in HEK cells expressing Na_v1.1, Na_v1.2, Na_v1.6, Na_v1.5, and Na_v1.7 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).

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.

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