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  5. Effects of a Diamide Compound on Voltage-Gated Sodium Channels in Rat Dorsal Root Ganglia

Effects of a Diamide Compound on Voltage-Gated Sodium Channels in Rat Dorsal Root Ganglia

来源 :中国上海第七届国际新药发明科技年会 | 被引量 : 0次 | 上传用户：only16666
【摘 要】
：
Voltage-gated sodium channels play a critical role in the excitability of nociceptors.The effect of a novel diamide compound,HYP-1,on tetrodotoxin sensitive (TTX-S) voltage-gated sodium channels in ra
【作 者】
：
Bohee Kang Yoo Lim Kam Jun-Mo Chung Hea-Young Park Choo 
【机 构】
：
School of Pharmacy,Ewha Womans University,Seoul,120-750,Korea
【出 处】
：
中国上海第七届国际新药发明科技年会
【发表日期】
：
2009年1期
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论文部分内容阅读
　　Voltage-gated sodium channels play a critical role in the excitability of nociceptors.The effect of a novel diamide compound,HYP-1,on tetrodotoxin sensitive (TTX-S) voltage-gated sodium channels in rat dorsal root ganglion (DRG) neurons were studied using whole-cell patch clamp electrophysiology.The blocking of sodium channels by HYP-1 was concentration dependent with IC50 value of 4.12 μM.HYP-1 blocked TTX-S sodium channel currents more in the negative voltage range than in the positive voltage range and shifted the voltage range which TTX-S current activation occurred.The ability of HYP-1 to attenuate sodium currents in DRG neurons suggests that this could be developed as novel analgesic to relieve chronic pain.
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