首页|呼吸抑制作用减弱的新型阿片类药物研究进展

呼吸抑制作用减弱的新型阿片类药物研究进展

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阿片类药物通过激动阿片受体,激活G蛋白、β-抑制蛋白等下游信号通路而发挥镇痛与麻醉效应,但引起的呼吸抑制是临床常见的严重问题。一直以来,阿片类药物基础和临床研究的目标之一是将镇痛作用与呼吸抑制作用分离,研发镇痛活性强、呼吸抑制作用减弱的新型阿片类药物。目前,外周选择性阿片受体激动剂、偏向性阿片受体激动剂、混合性阿片受体激动剂、内源性阿片肽和阿片受体剪接异构体激动剂等药物相继被研发,其中偏向性阿片激动剂奥赛利定(TRV130)已上市。随着研究的深入,将有更多新型阿片类药物用于临床治疗,以提高用药安全性。
Research progress in novel opioid drugs with reduced respiratory depression
Opioid drugs activate G protein and(or)β-arrestin protein signaling pathways by acting on opioid receptors,which can generate analgesia and anesthesia effects,but the accompanying respiratory depression is a serious and common clinical problem.Until now,one of the goals of the basic research and therapeutic application of opioid drugs is to separate the analgesic effect from the respiratory depression side effect,so as to develop new opioid drugs with strong analgesic activity and reduced respiratory depression side effect.At present,peripheral selective opioid agonists,biased opioid agonists,mixed opioid agonists,endogenous opioid peptides and opioid splicing variant agonists have been developed successively,of which the biased opioid agonist oliceridine(TRV130)has been marketed.As the research progresses,more new opioid drugs will be used in clinical treatment to improve drug safety.

analgesia,opioidsrespiratory depressionreceptors,opioidsbiased agonists

樊永正、韩丽君、赵亮

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联勤保障部队第九九一医院药剂科,湖北襄阳 441000

镇痛药,阿片类 呼吸抑制 受体,阿片样 偏向性激动剂

2024

中国新药与临床杂志
中国药学会 上海市食品药品监督管理局科技情报研究所

中国新药与临床杂志

CSTPCD北大核心
影响因子:0.967
ISSN:1007-7669
年,卷(期):2024.43(5)
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