J. Iñiguez-Lluhí

High potency μ-opioid receptor agonists engage sodium-bound receptor states.

The simple 2-state conformational selection model of G protein-coupled receptor activation suggests that, by binding to a high-affinity state, an agonist shifts receptor equilibrium in favor of active state (R∗) conformations that recruit heterotrimeric G proteins over inactive (R) conformations. Agonist binding affini...