Lu AE98134 T36813

Product Introduction
Bioactivity


英文名: Lu AE98134

描述: Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

体外活性: Lu AE98134 (30 μM) promotes the current mediated by Navv1.1 channel, and it activates Nav1.5 and to a lesser extent Nav1.2 but has no effect on Nav1.4, Nav1.6 and Nav1.7 currents in HEK cells expressing Nav1.1, Nav1.2, Nav1.6, Nav1.5, and Nav1.7 by step-wise depolarizing voltages using the whole-cell patchclamp configuration[1]. 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)[1].

体内活性: 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 NaV1.1 channels. The selective activation of FSINs by Lu AE98134 restores cognitive flexibility in adult Dlx5/6+/- mice[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 250 mg/mL (587.54 mM)


关键字: Lu AE98134 | Lu AE 98134 | Lu AE-98134

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