Pain management beyond opioids: a β-arrestin2-biased allosteric GPCR modulator opens new avenues for drug development
Abstract
A remarkable study by Guo et al., published in Cell , suggests a compelling new direction for improving pain management: biased allosteric modulation of the neurotensin receptor 1 (NTSR1), using the drug-like molecule SBI-810, promotes β-arrestin2 (βarr2) recruitment while avoiding canonical G protein signaling – thereby providing robust analgesia across a plethora of rodent models of both acute and chronic pain without impairing motor function, cognition, or causing opioid-like dependency. 1 , 2 SBI-810 is introduced as a highly promising molecule underscoring the therapeutic potential of biased and allosteric G protein-coupled receptor (GPCR) ligands to address an urgent unmet medical need.
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