Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor ( MOR ) antagonist with a K i of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor ( KOR ) ( K i = 4.9 nM) and delta-opioid receptor ( DOR ) ( K i = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction.
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