LAUSR

Opioids remain the most efficient medications against severe pain; they act on receptors that couple to heterotrimeric G‐proteins in the Gαi/o family. Opioids exert many of their acute effects through modulating ion channels via Gβγ subunits. Many of their side effects are attributed to β‐arrestin recruitment. Several biased agonists that do not recruit β‐arrestins, but activate G‐protein‐dependent pathways, have recently been developed. While these compounds have been proposed to be full agonists of G‐protein signalling in several high throughput pharmacological assays, their effects were not studied on ion channel targets.