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青蒿素衍生物对Na^+和K^+通道的抑制及其与普鲁卡因作用的比较 被引量:4
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作者 黄汾生 胡谦 施玉 《生理学报》 CAS CSCD 北大核心 1998年第2期145-152,共8页
抗疟新药青蒿素(Artemisinin)的某些含氮衍生物在动物实验中还显示局部麻醉效应。本工作利用分化的NG108-15细胞,在全细胞电压箝位下,比较了五种青篙素衍生物和普鲁卡因对电压门控钢流(INa)和延迟整流钾流(IK)的作用。所观察的... 抗疟新药青蒿素(Artemisinin)的某些含氮衍生物在动物实验中还显示局部麻醉效应。本工作利用分化的NG108-15细胞,在全细胞电压箝位下,比较了五种青篙素衍生物和普鲁卡因对电压门控钢流(INa)和延迟整流钾流(IK)的作用。所观察的五种衍生物均部分可逆地和剂量依赖地抑制INa,其中含芳香环的SM541作用最强,效应与普鲁卡因的相近。300μmol/L普鲁卡因对IK只有微弱的抑制作用;而五种衍生物在相同浓度下均明显抑制IK,并加快它的失活;其中除SM541外,还观察到在药物持续灌流下,对IK幅度的抑制效应迅速降低。 展开更多
关键词 青蒿素衍生物 普鲁卡因 钠通道 钾通道
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Effects of SO_(2)derivatives on sodium currents in acutely isolated rat hippocampal lead-exposed neurons 被引量:1
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作者 DU ZhengQing Lü GuoPing 《Science China(Life Sciences)》 SCIE CAS 2008年第9期802-807,共6页
In this study, the effects of acute SO_2 derivatives and chronic lead exposure together on sodium cur-rents (INa) were investigated in acutely isolated rat hippocampal neurons by using the whole-cell patch clamp techn... In this study, the effects of acute SO_2 derivatives and chronic lead exposure together on sodium cur-rents (INa) were investigated in acutely isolated rat hippocampal neurons by using the whole-cell patch clamp techniques. We found that chronic lead exposure hardly reduced the amplitudes of INa. In the normal condition, sodium current started to appear at around ?70 mV, and reached the peak current at around ?40 mV. After chronic lead exposure, the data changed to ?70 and ?30 mV. After adding SO2 derivatives, the data changed to ?80 and ?40 mV, respectively. SO_2 derivatives caused a significant in-crease of INa in hippocampal chronic-lead exposed neurons. Chronic lead exposure induced a right shift of the activation curve and a left shift of the inactivation curve of sodium channels. SO_2 derivatives caused negative shifts of the activation and inactivation curves of INa in hippocampal chronic-lead ex-posed neurons. Lead exposure put off the time reaching the peak of INa activation. SO_2 derivatives in-creased the time constants of inactivation after lead exposure. The interaction of lead and SO_2 deriva-tives with voltage-dependent sodium channels may lead to changes in electrical activity and contribute to worsening the neurotoxicological damage. 展开更多
关键词 SO_(2)derivatives LEAD hippocampal neurons whole-cell patch clamp techniques i_(na)
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