塞来昔布对心脏钠离子通道Nav 1.5电生理特性的影响

针对塞来昔布对与心脏毒性密切相关的钠离子通道Na_v1.5电生理特性的影响进行了研究.采用全细胞膜片钳技术，检测塞来昔布对Na_v1.5的电生理特性的影响，包括电流峰值、电压依赖性激活、电压依赖性失活以及恢复动力学.研究结果表明，塞来昔布对Na_v1.5的峰电流具有抑制作用，且呈浓度依赖性，其抑制作用的IC₅₀值为1.54×10^-8mol/L;塞来昔布促进了Na_v1.5的激活及失活过程，使其难以恢复到静息状态.塞来昔布对Na_v1.5峰电流的明显抑制作用，表明其潜在的心脏风险可能与Na_v1.5密切相关.

Effect of Celecoxib on Electrophysiological Property of Cardiac Sodium Channel Nav1.5

The effect of celecoxib on electrophysiological property of Na_v1.5 was studied，which was associated with cardiac toxicity. The effects of celecoxib on the electrophysiological properties of Na_v 1.5， including peak current， voltage-dependent activation， voltage-dependent inactivation and recovery kinetics， were investigated by whole cell patch clamp technique. The results showed that celecoxib inhibited the peak currents of Na_v1.5 in a concentration-dependent manner with a calculated IC₅₀ value of 1.54×10^-8mol/L. Moreover， celecoxib promoted the activation and inactivation phase of Na_v1.5， making it somewhat difficult to recover from the inactivation to the resting state. The prominent inhibition of celecoxib on Na_v1.5 indicated that there might be a close relationship between potential cardiovascular risks and Na_v1.5.