论文部分内容阅读
青蒿素的某些衍生物已被作为救治脑型和抗药性疟疾的首选药物应用于临床，其中，一个含氮的水溶性衍生物ＳＭ４８６在动物实验中显示局部麻醉效应。本文报告它对运动神经末梢的Ｎａ＋，Ｋ＋通道的作用．实验于小鼠胸三角肌标本上进行，借助于一水浸物镜在放大４００倍显微镜下将微电极插至表层神经束的周鞘下间隙，记录神经末梢膜电流。获得的结果为：（１）ＳＭ４８６对ⅠＮａ和ⅠＫ产生与剂量有关的抑制。抑制ⅠＫ的最小有效浓度较ⅠＮａ的低；（２）抑制是可逆的，既使在ⅠＮａ和ⅠＫ几乎完全被抑制的情况下，简单冲洗也可使之恢复；（３）ⅠＫ是逐渐降低的，而ⅠＮａ总是在ⅠＫ降低之后才迅速下降。在同样实验条件下普鲁卡因对ⅠＮａ和ⅠＫ有与上述ＳＭ４８６相似的作用，唯其有效浓度较高。
Certain derivatives of artemisinin have been used clinically as the drug of choice for the treatment of brain-type and drug-resistant malaria. Among them, a nitrogen-containing water-soluble derivative, SM486, shows a local anesthetic effect in animal experiments. This article reports its effect on Na +, K + channels in motor nerve endings. Experiments were performed on the mouse thoracic deltoid muscle samples. With the aid of an immersion objective, the microelectrode was inserted into the space under the perimeter of the superficial nerve sheath at a magnification of 400 times to record the nerve endings membrane current. The results obtained are: (1) SM486 produces dose-related inhibition of I Na and IK. The minimum effective concentration of inhibiting IK is lower than that of ⅠNa; (2) the inhibition is reversible, and even simple washing can restore it even when ⅠNa and ⅠK are almost completely inhibited; (3) ⅠK is gradually decreased, However, ⅠNa always decreased rapidly after the decrease of ⅠK. Under the same experimental conditions, procaine has similar effects to ⅠNa and ⅠK as SM486, except for its higher effective concentration.