MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor ( MOR ) antagonist, with an IC 50 of 28.37 nM, an EC 50 of 4.25 nM, and a K i of 0.18 nM against MOR . MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder.
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