CAJ | 학술논문

目的探讨甲硫氨酸脑啡肽（ MEK）经不同分子量聚乙二醇（ PEG）修饰对热板致痛小鼠镇痛效果的改善作用。方法分别尾静脉注射31μmol/kg MEK-Cys-NH2、mPEG2000和mPEG5000修饰MEK-Cys-NH2，测定55℃热板致痛小鼠给药前和给药后15、30、60、120 min的痛阈值；以给药前后痛阈值的差值数据比较各受试物给药前后、给药后各时间点的差异，分析镇痛效果。结果尾静脉注射mPEG5000修饰MEK-Cys-NH2镇痛表现有强于并长于MEK-Cys-NH2和mPEG2000修饰MEK-Cys-NH2趋势，在给药后120 min时痛阈值高于MEK-Cys-NH2和阳性对照药吗啡（ P＜0.0）。结论适当相对分子质量PEG修饰MEK可提高镇痛强度和药效维持时间，对改善其成药性具有积极意义。
목적탐토갑류안산뇌배태（ MEK）경불동분자량취을이순（ PEG）수식대열판치통소서진통효과적개선작용。방법분별미정맥주사31μmol/kg MEK-Cys-NH2、mPEG2000화mPEG5000수식MEK-Cys-NH2，측정55℃열판치통소서급약전화급약후15、30、60、120 min적통역치；이급약전후통역치적차치수거비교각수시물급약전후、급약후각시간점적차이，분석진통효과。결과미정맥주사mPEG5000수식MEK-Cys-NH2진통표현유강우병장우MEK-Cys-NH2화mPEG2000수식MEK-Cys-NH2추세，재급약후120 min시통역치고우MEK-Cys-NH2화양성대조약마배（ P＜0.0）。결론괄당상대분자질량PEG수식MEK가제고진통강도화약효유지시간，대개선기성약성구유적겁의의。
Objective To investigate the improvement effect to analgesic activity of met-enkephalin(PEG) modified by different molecular weight to the painful mice induced by hot plate .Methods Tail intravenous injection MEK-Cys-NH2 that modified by 31 μmol/kg of MEK-Cys-NH2 ,mPEG2000 and mPEG5000 separately,to measure the threshold of pain before treatment and after treatment 15,30,60,120 min on the painful mice induced by hot plate at 55 ℃;according to the difference date of pain threshold before and after treatment to compare the difference of test drugs with different treatment time point ,analyse the analgesic activity .Results It has the trend that the analgesic performance of mPEG5000 modified MEK-Cys-NH2 was stronger and longer than MEK-Cys-NH2 and mPEG2000 modified MEK-Cys-NH2 .The threshold of pain was higher than MEK-Cys-NH2 and the positive control drug morphine ( P<0.01) after treatment 120 min.Conclusions MEK modified by PEG with appropriate molecular weight could improve the strength of analgesic effect and the maintain time of drug efficacy ,and has positive significance to its druggability .