摘要
目的观察利多卡因和异丙酚对RAW264.7巨噬细胞P2X7受体电流的影响及两药之间的相互作用。方法应用小鼠RAW264.7巨噬细胞,采用全细胞膜片钳记录模式,记录ATP(100～5000μmol·L-1)诱发的P2X7受体电流。向细胞施加不同浓度的异丙酚(1～100μmol·L-1)或利多卡因(10～1000μmol·L-1),然后再施加2倍EC50水平的ATP。计算异丙酚或利多卡因对P2X7受体电流的IC50。向细胞先施加IC50水平异丙酚,再同时施加IC50水平的异丙酚与利多卡因(10～1000μmol·L-1),或向细胞先施加10μmol·L-1或1000μmol·L-1利多卡因,再同时施加相同浓度的利多卡因和IC50水平的异丙酚,观察异丙酚和利多卡因的相互影响。结果异丙酚或利多卡因可浓度依赖性的抑制2倍EC50ATP诱发的P2X7受体电流,异丙酚或利多卡因的IC50分别为(36.5±5.3)μmol·L-1和(223±34)μmol·L-1。先施加异丙酚后施加利多卡因300μmol·L-1或1000μmol·L-1可使P2X7受体电流幅度增强。先施加利多卡因后施加异丙酚对P2X7受体电流产生协同抑制作用。结论利多卡因和异丙酚可浓度依赖性的抑制巨噬细胞膜P2X7受体电流,在P2X7受体已受异丙酚抑制时,低浓度和高浓度的利多卡因对P2X7受体产生先抑制后兴奋的双向调节作用。
Aim To investigate the effects of propofol and lidoeaine on P2X7-gated currents and the interaction of both drugs. Methods RAW2647 macrophages were cultured, whole-cell patch clamp technique was used to record the P2XT-gated currents induced by ATP with two times EC50 level under 1 - 100 μmol · L^-1 propofol or 10 -1 000 μmol · L^-1 lidoeaine. Then, propofol of IC50 level and lidoeaine with 10 - 1 000 μmol ·L^-1 were administered, and the P2X7-gated currents were recorded. Results Propofol and lidocaine could inhibit P2X7-gated currents in a concentration-dependent manner, and the IC50 level was （36. 5 ± 5.3） μmol ·L^-1 and （223±34） μmol·L^-1, respectively. Lidocaine with high concentration （300 μmol · L ^- 1,1 000 μmol ·L^- 1 ） following the adminis- tration of propofol of EC50 level could increase the P2X7-gated currents （ P 〈 0. 05 ）, but propofol of EC50 level following the administration of lidocaine with low concentration （ 10 μmol · L^-1） or high concentration （1 000 μmol · L^-1） could generate synergistic inhibitory effect on P2X7-gated currents. Conclusions Propofol and lidocaine can inhibit P2X7-gated currents,and lidocaine within the range from 10 μmol ·L^-1 to 1 000 μmol· L^- 1following propofol administration can generate bidirectional effect on P2X7-gated currents.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2009年第7期911-914,共4页
Chinese Pharmacological Bulletin
基金
国家自然科学基金资助课题(No30471657)
