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NS8593 hydrochloride

CAS No. : 875755-24-1

MCE 站：NS8593 hydrochloride

产品活性：NS8593 hydrochloride 是一种有效的选择性的 SK channels (小电导钙激活钾通道)抑制剂。NS8593 hydrochloride 可逆地抑制 SK3 介导的电流，K_d 值为 77 nM。NS8593 hydrochloride 抑制所有 SK1-3 亚型的 Ca²⁺ 依赖性 (在 0.5 μM Ca²⁺ 时，K_d 分别为 0.42、0.60 和 0.73 μM)，并且不影响中间电导和大电导的钙激活钾通道 (分别为 hIK 和 hBK 通道)。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: When tested in excised patches, it is found that the inhibition by NS8593 (compound 14) decreased as the intracellular [Ca²⁺] is increased and that NS8593 is equipotent when applied from either the intracellular or the extracellular side of the cell membrane. A HEK293 cell transiently transfected with hSK3 channels is inhibited by 80% upon application of 100 nM apamin and by 75% after application of 300 nM NS8593. In contrast, NS8593 inhibits the mutated channel by 45% at 300 nM. NS8593 thus remains active on the apamin-insensitive SK3 channel, although the K_d value of 0.43 ?M is 4-fold higher than found for a wild-type hSK3 channel (K_d of 0.10 ?M). As the potency of NS8593 is dependent on the degree of SK3 channel activation, the decreased potency could thus reflect an increased apparent Ca²⁺-sensitivity of the mutated channels. Similar to the whole-cell experiments, the potency of NS8593 is reduced 3-fold from 0.67 ?M to 2.2 ?M when tested at a Ca²⁺ concentration of 500 nM.

In Vivo: NS8593 (compound 14) (3 and 10 mg/kg intravenously) is able to affect firing rate and firing pattern of dopaminergic neurons in vivo in C57Bl/6 mice.

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