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新的镇痛靶点及相应的镇痛先导化合物

Novel analgesic targets and corresponding analgesic leading compounds
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摘要 阿片类药物是常用的镇痛药物,但有很大的副作用,包括潜在的恢复延迟和永久性残疾的风险。本文综述了N-甲基-D-天冬氨酸受体、大麻素受体、前列腺素E2受体4受体和基质金属蛋白酶受体等镇痛靶点以及一些阻断疼痛信号通路的新靶点。此外,还描述了一些针对于这些靶点的新的激动剂、拮抗剂和具有激动剂(拮抗剂)活性的先导化合物。与传统类阿片类药物相比,这些新化合物通常具有良好的镇痛活性和较低的副作用,它们有望发展成为新的镇痛剂,并将为需要疼痛治疗的临床患者带来福音。 Opioid medications have been used for pain management,but there are negative side effects,including a potential delay in recovery and increased risk of permanent disability.In this paper,analgesic targets including N-methyl-D-aspartate receptors,cannabinoid receptors,prostaglandin E2 receptor 4 receptors,matrix metalloproteinase receptors,and some new targets for blocking pain signaling pathways associated with these receptors are reviewed.In addition,some novel agonists,antagonists,and leading compounds with agonistic(antagonistic)activities interacting with the target are also described.These novel compounds usually have better analgesic activity and lower side effects than traditional opioids.They are expected to be developed into new analgesics and benefit clin⁃ical patients who need pain treatment.
作者 郑博阳 曾瑞红 ZHENG Bo-yang;ZENG Rui-hong(Department of Immunology,Hebei Medical University,Shijiazhuang 050017,China)
出处 《中国药理学与毒理学杂志》 CAS 北大核心 2019年第12期1057-1065,共9页 Chinese Journal of Pharmacology and Toxicology
基金 国家自然科学基金(81671635) 国家自然科学基金(31240084)。
关键词 镇痛药 靶点 激动剂 拮抗剂 先导化合物 analgesic target agonist antagonist leading compound
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