| 1,6-二(4-苯乙基-1-甲基-1-哌嗪基)己烷二溴化物的镇痛活性研究 |
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| 引用本文： | 张红梅,李长龄,李润涛.1,6-二(4-苯乙基-1-甲基-1-哌嗪基)己烷二溴化物的镇痛活性研究[J].中国药理学通报,2003,19(3):303-305. |
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| 作者姓名： | 张红梅 李长龄 李润涛 |
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| 作者单位： | 1. 北京大学药学院药理学系,北京,100083
2. 北京大学药学院化学生物学系,北京,100083 |
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| 基金项目： | 国家自然科学基金资助课题No 2 9972 0 0 5 |
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| 摘 要： | 目的 研究哌嗪类新化合物 1,6 二 (4 苯乙基 1 甲基 1 哌嗪基 )己烷二溴化物 (97 9 G4 )的镇痛作用及机制。方法 通过醋酸扭体模型、热板、甩尾、纳洛酮拮抗试验及豚鼠回肠离体标本研究样品的镇痛活性及机制。结果 sc 97 9 G4 5mg·kg-1即可有效抑制小鼠扭体反应 (P <0 0 5 ) ,ID50为 8 8mg·kg-1;sc 4 0mg·kg-1、icv 2 5 μg·kg-1均可延长热板实验的舔足阈 (P <0 0 5 ) ;sc 2 0mg·kg-1可延长甩尾试验的潜伏期 (P <0 0 1) ;纳洛酮可拮抗其镇痛活性 ;97 9 G4可激动豚鼠回肠离体标本上的阿片受体。结论 97 9 G4具有的镇痛活性 ,主要作用部位在中枢 ,其镇痛活性可被纳洛酮拮抗 ,但作用特点有别于吗啡
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| 关 键 词： | 哌嗪类 1 6二(4苯乙基1甲基1哌嗪基)己烷二溴化物 镇痛 阿片受体 |
| 文章编号： | 1001-1978(2003)03-0303-04 |
| 修稿时间： | 2002年8月9日 |
Studies on analgesic effect of 1,6-Di-(4-phenethyl-1-methyl-1-piperazinyl) hexane dibromide |
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| ZHANG Hong Mei,LI Chang Ling,LI Run Tao.Studies on analgesic effect of 1,6-Di-(4-phenethyl-1-methyl-1-piperazinyl) hexane dibromide[J].Chinese Pharmacological Bulletin,2003,19(3):303-305. |
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| Authors: | ZHANG Hong Mei LI Chang Ling LI Run Tao |
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| Institution: | ZHANG Hong Mei,LI Chang Ling,LI Run Tao 1 |
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| Abstract: | AIM To investigate the analgesic effect of 1,6 Di (4 phenethyl 1 methyl 1 piperazinyl) hexane dibromide (97 9 G4) and its mechanisms. METHODS The writhing model of mice induced by acetic acid, hot plate test (sc, icv), tail flick test and the model of electrical stimulation induced contraction of guinea pig ileum were used. RESULTS The inhibition of writhing reaction induced by acetic acid was found (ID 50 =8 8 mg·kg -1 ) and the rising of mice pain threshold in hot plate test and in tail flick test was obvious ( P <0 05). And the analgesic effect of 97 9 G4 could be antagonized by naloxone. In addition, the inhibition of guinea pig ileum contraction induced by electric stimulation was observed (IC 50 =39 8 μmol·L -1 ). CONCLUSION The analgesic effects of 97 9 G4 was significant and could be antagonized by naloxone. The action characteristic is not just the same as morphine. |
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| Keywords: | piperazines 1 6 Di (4 phenethyl 1 methyl 1 piperazinyl)hexane dibromide analgesia opioid receptor |
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