The inhibitory effects of nifedipine on outward voltage-gated potassium currents in mouse neuroblastoma N2A cells

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• 作者：Xiao-Yue Qiu^a ; Kai Li^a ; Xiao-Qing Li^b ; Xian-Tao Li^b ; ^{li56567@yeah.net" class="auth_mail" title="E-mail the corresponding author}
• 关键词：N2A cells ; Nifedipine ; Kv currents ; Voltage-dependent manner
• 刊名：Pharmacological Reports
• 出版年：2016
• 出版时间：June 2016
• 年：2016
• 卷：68
• 期：3
• 页码：631-637
• 全文大小：805 K

文摘

Voltage-gated K⁺ (Kv) channels have a pivotal role in tuning the action potential duration and excitability in neuronal cells. Although Ca²⁺ channel antagonist nifedipine exhibited an inhibitory effect on cardiac Kv currents, a possible action of nifedipine on neuronal Kv currents has not been fully investigated.

Methods

The effects of nifedipine on elicited Kv currents were characterized using whole-cell recording in mouse neuroblastoma N2A cells.

Results

Exposure to nifedipine induced a dose-dependent inhibition of Kv currents with an IC₅₀ value of 22.3 ± 4.2 μM and prolonged the time course of activation. The half-maximum activation potential was 1.6 ± 1.7 mV in control conditions and became 13.5 ± 1.5 mV in 50 μM nifedipine. In addition, the decay rate of Kv currents was substantially accelerated by 39.5% at +60 mV. For the voltage-dependent inactivation, the half-maximum inactivation potential was −13.8 ± 0.8 mV and strongly shifted to the left following treatment with 50 μM nifedipine.

Conclusion

Treatment with nifedipine exerted a strong influence on the activation and inactivation rate of Kv currents as well as an obvious leftward shift in the inactivation curve. These data indicated that nifedipine exerted an inhibitory effect on Kv currents in N2A cells.