阿片受体与吗啡耐受研究进展
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- 英文论文题名：Progress in Opioid Receptor and Morphine Tolerance
- 论文作者：刘明 ; 胡文祥
- 英文论文作者：Ming Liu ; Wenxiang Hu ; College of Life Sciences ; Capital Normal University ; Chinese People's Liberation Army Strategic Support Troops ; Space Systems Division
- 年：2016
- 作者机构：首都师范大学生命科学学院;中国人民解放军战略支援部队航天系统部;
- 论文关键词：μ型阿片受体 ; 吗啡耐受 ; 镇痛
- 英文论文关键词：Mu opioid receptor ; morphine tolerance ; analgesia
- 会议召开时间：2016-07-01
- 会议录名称：中国化学会第30届学术年会摘要集-第三十四分会：公共安全化学
- 语种：中文
- 分类号：TQ460.1
- 学会代码：ZGHY
- 会议名称：中国化学会第30届学术年会-第三十四分会 ; 公共安全化学
- 会议地点：中国辽宁大连
- 主办单位：中国化学会
- 学会名称：中国化学会
- 页数：1
- 文件大小：184k
- 原文格式：D
- 会议级别：全国
摘要
阿片受体介导了镇痛、催眠、镇咳、呼吸抑制、缩瞳和呕吐,μ型阿片受体(MOR)数量的降低是产生吗啡耐药的重要原因之一。基于阿片受体激动剂(如吗啡)的耐受性,在连续使用该类药物后,还会导致药物的成瘾性,体内外实验也表明吗啡诱导能使MOR下调。在MOR介导的细胞信号转导和分子水平方面对吗啡耐受机制的研究都取得了进展。Stoicea N等报道临床上使用阿片受体激动剂治疗慢性痛病人时,该类病人可能会出现阿片类药物诱导的痛觉超敏现象,即吗啡耐受作用,适宜剂量的γ-氨基丁酸类似物加巴喷丁能够降低这一现象的发生率,从而减少阿片类用药量。大麻素受体2(CB2)参与吗啡耐受的发生与发展。CB2受体选择性激活剂与吗啡联合使用,可以减弱吗啡诱导产生的痛觉过敏和异常疼痛,抑制吗啡耐受的发生与发展。吗啡与小剂量阿片拮抗剂合用,吗啡与小剂量芬太尼合用,可明显减少耐受的发生。
Opiates are the most common clinical used drugs, exciting opioid receptors in the central nervous system, mediate analgesic, hypnotic, antitussive, respiratory depression, miosis and vomiting effect.The reduction of the Mu opioid receptor(MOR) number is one of the important reasons to produce morphine tolerance. After continuous use of drugs, opioid receptor agonists may lead to drug addiction.Many in vivo, in vitro studies show that morphine may down-regulate the level of MOR. The study of the mechanisms of morphine tolerance in the MOR-mediated signal transduction and molecular level, have made some progress. Stoicea N etal reported that when using opioid receptor agonist treating chronic pain patients, patients may appear clinically opioid-induced allodynia phenomenon that morphine tolerance. Suitable doses of γ-aminobutyric acid analogs of gabapentin can reduce the incidence of this phenomenon, thereby reducing the amount of opioid medication.Cannabinoid receptor 2 selective activator used in combination with morphine can weaken induced hyperalgesia and allodynia, inhibit the occurrence and development of morphine tolerance. Morphine in combination with low-dose opioid antagonist, morphine and fentanyl combination, can significantly reduce the occurrence of tolerence.
Opiates are the most common clinical used drugs, exciting opioid receptors in the central nervous system, mediate analgesic, hypnotic, antitussive, respiratory depression, miosis and vomiting effect.The reduction of the Mu opioid receptor(MOR) number is one of the important reasons to produce morphine tolerance. After continuous use of drugs, opioid receptor agonists may lead to drug addiction.Many in vivo, in vitro studies show that morphine may down-regulate the level of MOR. The study of the mechanisms of morphine tolerance in the MOR-mediated signal transduction and molecular level, have made some progress. Stoicea N etal reported that when using opioid receptor agonist treating chronic pain patients, patients may appear clinically opioid-induced allodynia phenomenon that morphine tolerance. Suitable doses of γ-aminobutyric acid analogs of gabapentin can reduce the incidence of this phenomenon, thereby reducing the amount of opioid medication.Cannabinoid receptor 2 selective activator used in combination with morphine can weaken induced hyperalgesia and allodynia, inhibit the occurrence and development of morphine tolerance. Morphine in combination with low-dose opioid antagonist, morphine and fentanyl combination, can significantly reduce the occurrence of tolerence.
引文
[1]Song XJ.Chinese Journal of Pain Medicine,2016,22(1):2-7