江汉大学学报：自然科学版
江漢大學學報：自然科學版
강한대학학보：자연과학판
Journal of Jianghan University:Natural Sciences
2011年
3期
61-66
,共6页
bis(7)-tacrine%NMDA%海马%二硫苏糖醇%精胺%镁%锌%MK-801
bis(7)-tacrine%NMDA%海馬%二硫囌糖醇%精胺%鎂%鋅%MK-801
bis(7)-tacrine%NMDA%해마%이류소당순%정알%미%자%MK-801
bis（7）-tacrine%NMDA%hippocampus%dithiothreitol%spermine%Mg2＋%Zn2＋%MK-801
目的：研究新型tacrine双联体bis（7）-tacrine对NMDA受体的作用位点.方法：大鼠海马神经元原代培养,全细胞膜片钳记录培养大鼠海马神经元上NMDA激活电流变化.结果：细胞外液pH值从8.1改变到6.7,在细胞外液中加入二硫苏糖醇（2 mmol/L）、精胺（10 mol/L）、镁离子（50～500 mol/L）或锌离子（5～20 mol/L）均不引起bis（7）-tacrine对NMDA电流抑制率的改变.电极内液中加入5 mol/L bis（7）-tacrine也未观察到外加的0.5 mol/L bis（7）-tacrine对30 mol/L NMDA激活电流抑制率的改变.0.5 mol/L bis（7）-tacrine及1 mol/L dizocilpine（MK-801）分别对30 mol/L NMDA激活电流抑制了36%和22%,而在两种药物都存在的条件下,30 mol/L NMDA电流仅被抑制了37%.结论：bis（7）-tacrine虽然不大可能作用于MK-801位点,但MK-801和bis（7）-tacrine之间可能存在着相互的负性调节作用.
目的：研究新型tacrine雙聯體bis（7）-tacrine對NMDA受體的作用位點.方法：大鼠海馬神經元原代培養,全細胞膜片鉗記錄培養大鼠海馬神經元上NMDA激活電流變化.結果：細胞外液pH值從8.1改變到6.7,在細胞外液中加入二硫囌糖醇（2 mmol/L）、精胺（10 mol/L）、鎂離子（50～500 mol/L）或鋅離子（5～20 mol/L）均不引起bis（7）-tacrine對NMDA電流抑製率的改變.電極內液中加入5 mol/L bis（7）-tacrine也未觀察到外加的0.5 mol/L bis（7）-tacrine對30 mol/L NMDA激活電流抑製率的改變.0.5 mol/L bis（7）-tacrine及1 mol/L dizocilpine（MK-801）分彆對30 mol/L NMDA激活電流抑製瞭36%和22%,而在兩種藥物都存在的條件下,30 mol/L NMDA電流僅被抑製瞭37%.結論：bis（7）-tacrine雖然不大可能作用于MK-801位點,但MK-801和bis（7）-tacrine之間可能存在著相互的負性調節作用.
목적：연구신형tacrine쌍련체bis（7）-tacrine대NMDA수체적작용위점.방법：대서해마신경원원대배양,전세포막편겸기록배양대서해마신경원상NMDA격활전류변화.결과：세포외액pH치종8.1개변도6.7,재세포외액중가입이류소당순（2 mmol/L）、정알（10 mol/L）、미리자（50～500 mol/L）혹자리자（5～20 mol/L）균불인기bis（7）-tacrine대NMDA전류억제솔적개변.전겁내액중가입5 mol/L bis（7）-tacrine야미관찰도외가적0.5 mol/L bis（7）-tacrine대30 mol/L NMDA격활전류억제솔적개변.0.5 mol/L bis（7）-tacrine급1 mol/L dizocilpine（MK-801）분별대30 mol/L NMDA격활전류억제료36%화22%,이재량충약물도존재적조건하,30 mol/L NMDA전류부피억제료37%.결론：bis（7）-tacrine수연불대가능작용우MK-801위점,단MK-801화bis（7）-tacrine지간가능존재착상호적부성조절작용.
Objective：To study the modulatory site of bis（7）-tacrine on NMDA receptors.Methods：The effect of bis（7）-tacrine on NMDA-activated currents was investigated using whole-cell patch-clamp recording in cultured rat hippocampal neurons in the absence and presence of different NMDA receptor modulaters.Results：The inhibitory rates NMDA-activated currents by bis（7）-tacrine were neither altered by changing extracellular pH（pH 8.1～6.7）,nor by adding dithiothreitol（2 mmol/L）,spermine（10 mol/L）,Mg2＋（50～500 mol/L）,or Zn2＋（5～20 mol/L） to the external solution.5 mol/L bis-tacrine in the recording pipette solution did not alter the inhibition rate of 30 mol/L NMDA-activated current by 0.5 mol/L bis（7）-tacrine applied externally.0.5 mol/L bis（7）-tacrine and 1 mol/L dizocilpine（MK-801） inhibited NMDA-activated currents by 36 % and 22 %,respectively;co-application of these two drugs only inhibited NMDA-activated current by 37 %.Conclusion：Although bis（7）-tacrine is very unlikely acting at the MK-801 site,MK-801 and bis（7）-tacrine may negatively modulate the inhibition of NMDA receptor function with each other.
