Emerging Field of Biased Opioid Agonists
Highlights
- The core concept of ligand bias is that some agonists, particularly at GPCRs, can stabilize different active conformations of the receptor than other agonists resulting in variable downstream molecular signals, and thus effects.5 For opioids, this concept refers to variable downstream signaling, given that the activation of opioid GPCRs triggers 2 main transducing pathways, G proteins and GPCR kinases/β-arrestins (View Highlight)
- opioid receptors are GPCRs with 3 subtypes: delta (δ), kappa (κ), and mu (μ). In clinical practice, most opioid agonists target μ-opioid receptors which, when activated, result in both G protein and β-arrestin signaling (View Highlight)