中国药房2024，Vol.35Issue(17)：2176-2180,5.DOI:10.6039/j.issn.1001-0408.2024.17.21
新型阿片类镇痛药的研发进展
Research progress of novel opioid analgesics
摘要
Abstract
Opioid analgesics are currently known as the best analgesics.However,toxicity and side effects such as constipation,tolerance and addiction severely limit their clinical application.With the in-depth understanding of the signal transduction mechanism of opioid receptors and the continuous advancement of drug design technology,researchers have managed to develop many promising new methods to get low-toxic and more efficient opioid analgesics,which are different from the traditional morphine skeleton structure modifications.This article focuses on three new research strategies of G-protein biased activation,"one drug-multiple targets"and peripheral activation.The basic principles of relative separation of analgesic activity and adverse drug reaction by each strategy are introduced,and the latest research progress of representative drugs is briefly reviewed.Among them,the recently approved novel opioid analgesics oliceridine and tegileridine are G-protein biased μ-opioid receptor agonists,Cebranopadol is a typical"one drug-multiple targets"analgesic,and NFEPP is a representative drug of peripheral opioid receptor agonists.The above several strategies complement each other and provide reference for the development of new opioid analgesic drugs.关键词
阿片类镇痛药/偏向性激动剂/一药多靶/外周激动剂/新药研发Key words
opioid analgesic/biased agonist/one drug-multiple targets/peripheral agonist/new drug development分类
药学引用本文复制引用
贺春波,王丹,杨淑佳,周开文,邓怡平,董守良..新型阿片类镇痛药的研发进展[J].中国药房,2024,35(17):2176-2180,5.基金项目
山东省自然科学基金项目(No.ZR2023QH304) （No.ZR2023QH304）
德州学院科学研究基金项目(No.2021xjrc212) （No.2021xjrc212）
