中国药理学与毒理学杂志2024，Vol.38Issue(7)：481-495,15.DOI:10.3867/j.issn.1000-3002.2024.07.001
低成瘾性阿片类镇痛药物研发现状和趋势
Developments of opioid analgesics with low addiction potential
摘要
Abstract
Opioid analgesics play an important role in pain management.While opioid analgesics have been used to control various types of acute and chronic pain,they bring about the risks of non-medical use and addiction,which results in a worldwide opioid crisis.Opioid receptors are widely distributed in the central nervous system and mediate complex biological effects.The side effects of opioid analgesics,such as respiratory depression,dependence and addiction,have severely limited their clinical applications.The main strategies for developing new opioid analgesics with low addiction potential involve abuse-deterrent formulations,agonists targeting peripheral opioid receptors,G protein signaling-biased agonists of opioid receptors,agonists targeting opioid receptor heteromers and multi-functional ligands of opioid receptors.Most of them are undergoing clinical or pre-clinical research,and some new formulation medicines have been approved for marketing.Despite the analgesic or other therapeutic benefits,these strategies retain to some extent the potential risk of abuse and other adverse effects like to traditional opioid analgesics.How to fully separate the analgesic action from addiction potential remains challenging.Therefore,more efforts are needed to develop new opioid anal-gesics with low addiction potential.关键词
阿片类镇痛药物/疼痛/治疗/药物滥用/防滥用制剂/偏向激动/异聚体/多功能配体Key words
opioid analgesics/pain/treatment/drug abuse/abuse-deterrent opioid formulations/biased agonism/heteromers/multi-functional ligands分类
医药卫生引用本文复制引用
王志媛,吴宁..低成瘾性阿片类镇痛药物研发现状和趋势[J].中国药理学与毒理学杂志,2024,38(7):481-495,15.基金项目
国家自然科学基金(81874310) National Natural Science Foundation of China(81874310) （81874310）
