| 一种新的阿片受点不可逆激动剂7α-二(β-氯乙基)胺甲基-6,14-乙烯撑基四氢奥利文的药理研究 |
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| 引用本文： | 李建国,李灵源,金荫昌,虞鑫红,刘懋勤.一种新的阿片受点不可逆激动剂7α-二(β-氯乙基)胺甲基-6,14-乙烯撑基四氢奥利文的药理研究[J].药学学报,1989,24(5):321-325. |
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| 作者姓名： | 李建国 李灵源 金荫昌 虞鑫红 刘懋勤 |
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| 作者单位： | 中国医学科学院基础医学研究所,北京100730;**上海医科大学药学院,上海200032 |
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| 摘 要： | α-CAM是一新的阿片受点不可逆激动剂,在离体组织(GPI,MVD,RVD和RbVD)及大鼠脑P2膜制备上均表现不可逆作用。对小鼠镇痛(icv)ED50为0.12 nmol/鼠,镇痛作用可持续2～3 d,是迄今所知镇痛时间最长的化合物。一次注射(icv)即可使小鼠成瘾,可作为研究成瘾机理的工具药。
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| 关 键 词： | 阿片受点 不可逆激动剂 7α-二(β-氯乙基)胺甲基-6 14-乙烯撑基四氢奥利文 镇痛药 成瘾 |
| 收稿时间： | 1988-02-02 |
Pharmacological study on a new irreversible agonist of opioid receptors, 7 alpha-bis(beta-chloroethyl) aminomethyl-6, 14-endoetheno-tetrahydrooripavine |
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| JG Li,LY Li,YC Jin,XH Yu and MQ Liu.Pharmacological study on a new irreversible agonist of opioid receptors, 7 alpha-bis(beta-chloroethyl) aminomethyl-6, 14-endoetheno-tetrahydrooripavine[J].Acta Pharmaceutica Sinica,1989,24(5):321-325. |
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| Authors: | JG Li LY Li YC Jin XH Yu and MQ Liu |
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| Abstract: | 7 alpha-bis (beta-chloroethyl) aminomethyl-6, 14-endoetheno-tetrahydro oripavine (alpha-CAM) is a new irreversible opioid receptor agonist. Its effect on isolated tissues (guinea pig ileum, mouse vas deferens, rat vas deferens and rabbit vas deferens) were studied. It was shown to be bound irreversibly to rat brain P2 membrane preparations. The ED50 of its analgesic effect in mice (icv) was found to be 0.12 nmol/mouse, and the effect may last as long as 2-3 days. It is a compound which produces the longest analgesia known up to date. A single dose (icv) of alpha-CAM was sufficient to produce dependence in mice. Thus, the compound may serve as an agent for studying the mechanism of physical dependence. |
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| Keywords: | Irreversible agonist 7α-bis (β-chloroethyl) aminomethyl-6 14-endothenotetrahydrooripavine (α-CAM) Analgesic Dependence Opioid receptors |
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