Heteromers of μ-δ opioid receptors: new pharmacology and novel therapeutic possibilities
作者： Wakako Fujita , Ivone Gomes , Lakshmi A Devi
DOI: 10.1111/BPH.12663
关键词:
摘要: Several studies suggest that heteromerization between μ (MOP) and δ (DOP) opioid receptors modulates the signalling properties of individual receptors. For example, whereas activation MOP by an agonist induces G protein-mediated signalling, same β-arrestin-mediated in context MOP-DOP receptor heteromer. Moreover, heteromer-mediated is allosterically modulated a combination DOP ligands. This has implications analgesia given morphine-induced antinociception can be potentiated Recently reagents selectively targeting heteromer such as bivalent ligands, antibodies or membrane permeable peptides have been generated; these are enabling to elucidate contribution endogenously expressed heteromers well development side-effects associated with chronic use. Recent advances drug screening technology led identification heteromer-biased activates both signalling. this exhibits potent antinociceptive activity but reduced side-effects, suggesting ligands form basis for novel therapeutics treatment pain. In review, we summarize findings regarding biological functional characteristics vitro vivo heteromer-selective ligands. LINKED ARTICLES This article part themed section on Opioids: New Pathways Functional Selectivity. To view other articles visit http://dx.doi.org/10.1111/bph.2015.172.issue-2
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