Antinociception, tolerance and withdrawal symptoms induced by 7-hydroxymitragynine, an alkaloid from the Thai medicinal herb Mitragyna speciosa
Antinociception, tolerance and withdrawal symptoms induced by 7-hydroxymitragynine, an alkaloid from the Thai medicinal herb Mitragyna speciosa
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DOI：
10.1016/j.lfs.2004.10.086
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发表时间：
2005-11-19
期刊：
影响因子：
6.1
通讯作者：
Watanabe, K
中科院分区：
文献类型：
--
作者：
Matsumoto, K;Horie, S;Watanabe, K
7-羟基米特拉宁是从泰国药用植物铁线莲中分离得到的一种有效的阿片类镇痛生物碱，在本研究中，我们研究了与该化合物镇痛作用有关的阿片受体亚型。我们测试了长期服用7-羟基米曲宁的小鼠是否观察到耐受性的形成、对吗啡的交叉耐受性和纳洛酮诱导的戒断症状。皮下(S.C.)给予7-羟基米曲宁主要通过激活Mu-阿片受体产生有效的抗伤害性作用。与吗啡一样，对7-羟基米拉宁的抗伤害作用产生耐受性，对7-羟基米曲宁耐受的小鼠对吗啡有明显的交叉耐受性，反之亦然。纳洛酮诱导的戒断症状在长期服用7-羟基米曲宁或吗啡的小鼠中也同样出现。7-羟基米曲宁通过激活Mu-阿片受体和类吗啡药理特性显示出较强的抗伤害性作用，但7-羟基米曲宁在结构上不同于吗啡。7-羟基硝基呋喃的这些有趣的特性促进了对其作为阿片类药物研究的新型先导化合物的进一步研究，(C)2005年Elsevier Inc.保留所有权利。
7-Hydroxymitragynine is a potent opioid analgesic alkaloid isolated from the Thai medicinal herb Mitragyna speciosa, In the present study, we investigated the opioid receptor subtype responsible for the analgesic effect of this compound, [it addition. we tested whether development of tolerance, cross-tolerance to morphine and naloxone- induced withdrawal signs were observed in chronically 7-hydroxymitragynine-treated mice. Subcutaneous (s.c.) administration of 7-hydroxymitragynine produced a potent antinociceptive effect mainly through activation of mu-opioid receptors. Tolerance to the antinociceptive effect of 7-hydroxymitragynine developed as occurs to morphine, Cross-tolerance to morphine was evident in mice rendered tolerant to 7-hydroxymitragynine and vice versa. Naloxone-induced withdrawal signs were elicited equally in mice chronically treated with 7-hydroxymitragynine or morphine. 7-Hydroxymitragynine exhibited a potent antinociceptive effect based on activation of mu-opioid receptors and its morphine-like pharmacological character, but 7-hydroxymitragynine is structurally different from morphine. These interesting characters of 7-hydroxymitragynine promote further investigation of it as a novel lead compound for opioid studies, (c) 2005 Elsevier Inc. All rights reserved.