神经药理学报››2018,Vol. 8››Issue (2): 1-7.DOI:10.3969/j.issn.2095-1396.2018.02.001
• 专家论坛 •下一篇
孙毅,谭博,苏瑞斌
出版日期:
2018-04-26发布日期:
2018-04-16通讯作者:
谭博,男,助理研究员;研究方向:神经精神药理学;Tel:+86-010-66874604,E-mail:whutanbo@gmail.com 苏瑞斌,男,研究员;研究方向:神经精神药理学;Tel:+86-010-66931601,E-mail:ruibinsu@126.com作者简介:
孙毅,女,博士研究生;研究方向:神经精神药理学;Tel:+86-010-66874604,E-mail:surisun@yeah.net基金资助:
国家自然科学基金项目(No. 81773709)
SUN Yi,TAN Bo,SU Rui-bin
Online:
2018-04-26Published:
2018-04-16Contact:
谭博,男,助理研究员;研究方向:神经精神药理学;Tel:+86-010-66874604,E-mail:whutanbo@gmail.com 苏瑞斌,男,研究员;研究方向:神经精神药理学;Tel:+86-010-66931601,E-mail:ruibinsu@126.comAbout author:
孙毅,女,博士研究生;研究方向:神经精神药理学;Tel:+86-010-66874604,E-mail:surisun@yeah.netSupported by:
国家自然科学基金项目(No. 81773709)
摘要:吗啡等阿片类药物作为镇痛药应用已有数百年历史,但其致呼吸抑制、耐受和成瘾等副作用限制了该类药物的使用,因此人们一直致力于寻找副作用更低的新型镇痛药。近年研究发现,μ阿片受体下游除了经典的G 蛋白依赖型通路外,还独立存在由β-arrestin 介导的信号通路,吗啡激活μ阿片受体产生的镇痛、镇静效应主要通过G 蛋白依赖型通路介导,而胃肠功能紊乱、呼吸抑制、耐受等副反应则由β-arrestin 依赖型通路介导。如果能发现只激活G 蛋白依赖型通路而不激活β-arrestin 依赖型通路的偏向性配体,就可能得到镇痛效应强而副作用低的化合物,这为设计新型强效、低副作用的阿片类镇痛药提供了新思路。该文将对μ阿片受体下游β-arrestin 依赖型信号通路及偏向性配体的发现、发展和应用进行综述。
中图分类号:
孙毅,谭博,苏瑞斌.偏向性配体——阿片类镇痛药设计新思路[J]. 神经药理学报, 2018, 8(2): 1-7.
SUN Yi,TAN Bo,SU Rui-bin.Biased Ligand——Novel Paradigm for Opioid Analgesics[J]. Acta Neuropharmacologica, 2018, 8(2): 1-7.
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