|星空彩票电脑版 %A SUN Yi,TAN Bo,SU Rui-bin %T Biased Ligand——Novel Paradigm for Opioid Analgesics%0 Journal Article %D 2018 %J ACTA NEUROPHARMACOLOGICA %R 10.3969/j.issn.2095-1396.2018.02.001 %P 1-7 %V 8 %N 2 %U {http://actanp.hebeinu.edu.cn/CN/abstract/article_410.shtml} %8 2018-04-26 %X Morphine and related opioids have been used as clinical analgesics for centuries,but various side effects-which include respiratory depression,tolerance and addictionset a limit to medication. Consequently,unremitting efforts have been directed towards the discovery of effective and nonlethal pain killers. Recent studies identified a novel β-arrestindependent pathway through μ-opioid receptor and indicated that side effects of morphine are mediated through β-arrestin-dependent pathway while G-protein-dependent pathway is thought to confer analgesia,which means biased ligands to G-protein signaling are possible analgesics without side effects. The theory of biased ligands may provide a novel strategy to design better and safer opioid analgesics. In this review,we summarized the discovery,development and application of β-arrestin-dependent pathway and biased ligands.
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