Kappa Opioid Receptor Agonist and Brain Ischemia.
Kappa Opioid Receptor Agonist and Brain Ischemia.
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发表时间：
2014
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通讯作者：
Chunhua Chen;Chunhua Xi;Sugita Megumi;Liu Renyu
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作者：
Chunhua Chen;Chunhua Xi;Sugita Megumi;Liu Renyu
阿片受体，尤其是κ阿片受体（KOR）在脑缺血再灌注损伤的病理生理过程中起重要作用。以前公认的KOR激动剂活性包括抗伤害感受、心血管、抗过敏、利尿和镇咳作用，而来自各种缺血动物模型的令人信服的证据表明KOR激动剂通过各种机制具有神经保护作用。本文就KOR激动剂的性质及其在全脑和局灶性脑缺血中的作用作一综述。基于目前的临床前研究，KOR激动剂可用作神经保护剂。新近发现的高选择性非阿片类KOR激动剂salvinorin A为研究KOR在脑HI损伤中的作用及KOR激动剂的保护作用提供了新的工具。鼠尾草素A的独特药理学特征沿着人类使用的长期历史提供了其作为脑HI损伤的潜在替代药物的高度候选性。
Opioid receptors, especially Kappa opioid receptor (KOR) play an important role in the pathophysiological process of cerebral ischemia reperfusion injury. Previously accepted KOR agonists activity has included anti-nociception, cardiovascular, anti-pruritic, diuretic, and antitussive effects, while compelling evidence from various ischemic animal models indicate that KOR agonist have neuroprotective effects through various mechanisms. In this review, we aimed to demonstrate the property of KOR agonist and its role in global and focal cerebral ischemia. Based on current preclinical research, the KOR agonists may be useful as a neuroprotective agent. The recent discovery of salvinorin A, highly selective non-opioid KOR agonist, offers a new tool to study the role of KOR in brain HI injury and the protective effects of KOR agonist. The unique pharmacological profile of salvinorin A along with the long history of human usage provides its high candidacy as a potential alternative medication for brain HI injury.