MP1202

Description

MP1202 is a dual-functional agonist of MOR and KOR with EC50s of 0.32 and 0.13 ??M for mMOR-1 and mKOR-1, respectively. MP1202 has functional selectivity with reduction of ?-arrestin1/2 recruitment but significant activation of G-protein and G?-subtype at hMOR and hKOR. MP1202 has potent antinociceptive effects without typical opioid side effects, but it shows conditioned place preference and aversion behaviors in subtype-selective opioid KO mice model, promising for analgesia research.