Biased Ligand——Novel Paradigm for Opioid Analgesics

doi:10.3969/j.issn.2095-1396.2018.02.001

Abstract

Abstract: 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.

Key words: biased ligands, &, mu, opioid receptor, signal transduction, analgesic

CLC Number:

R964

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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