MP1202 is a dual agonist for MOR and KOR, with EC50 values of 0.32 µM for mMOR-1 and 0.13 µM for mKOR-1. It exhibits functional selectivity by reducing beta-arrestin1/2 recruitment in hMOR and hKOR while significantly activating G protein and Galpha subtypes. In opioid receptor subtype knockout mouse models, MP1202 demonstrates potent antinociceptive effects without typical opioid side effects, albeit it induces conditioned place preference and aversion behaviors, indicating potential for analgesic research.
Molekulargewicht:
556.44
CAS Nummer:
[2578974-82-8]
Formel:
C27H29IN2O3
Target-Kategorie:
Arrestin|||Opioid Receptor
T211669
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