Methocinnamox is a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. It binds non-covalently to the orthosteric site of the MOR in a pseudo-irreversible manner, leading to sustained receptor blockade until new receptors are synthesized. Additionally, Methocinnamox serves as a reversible antagonist at both kappa-opioid (KOR) and delta-opioid receptors (DOR), with Ki values of 4.9 nM and 2.2 nM, respectively, without exhibiting intrinsic agonist activity. This compound is applicable in research focused on opioid overdose reversal and addiction prevention.
Methocinnamox is a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. It binds non-covalently to the orthosteric site of the MOR in a pseudo-irreversible manner, leading to sustained receptor blockade until new receptors are synthesized. Additionally, Methocinnamox serves as a reversible antagonist at both kappa-opioid (KOR) and delta-opioid receptors (DOR), with Ki values of 4.9 nM and 2.2 nM, respectively, without exhibiting intrinsic agonist activity. This compound is applicable in research focused on opioid overdose reversal and addiction prevention.
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