117339-76-1
Chemical Structure
Methocinnamox
Synonym(s): M-CAM
- CAS No.: 117339-76-1
- Formula:C30H32N2O4
- Molecular Weight:484.59
IUPAC Name: (E)-N-((4R,4aS,7aR,12bR)-3-(cyclopropylmethyl)-9-hydroxy-7-oxo-1,2,3,4,5,6,7,7a-octahydro-4aH-4,12-methanobenzofuro[3,2-e]isoquinolin-4a-yl)-3-(p-tolyl)acrylamide
InChIKey: PJOHVEQSYPOERL-SHEAVXILSA-N
SMILES: O=C(CC1)[C@]([C@@](C2=C(C[C@H]3N4CC5CC5)C=C6)(CC4)[C@@]13NC(/C=C/C7=CC=C(C)C=C7)=O)([H])OC2=C6O
Biological Activity: Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki 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) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 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[1][2][3].
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Methocinnamox | Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki 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) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 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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References
- [1]. Gerak LR, et al. Methocinnamox Produces Long-Lasting Antagonism of the Behavioral Effects of µ-Opioid Receptor Agonists but Not Prolonged Precipitated Withdrawal in Rats. J Pharmacol Exp Ther. 2019 Nov;371(2):507-516. [Content Brief]
- [2]. Jimenez VM Jr, Castaneda G, France CP. Methocinnamox Reverses and Prevents Fentanyl-Induced Ventilatory Depression in Rats. J Pharmacol Exp Ther. 2021 Apr;377(1):29-38. [Content Brief]
- [3]. Maguire DR, France CP. Behavioral pharmacology of methocinnamox: A potential new treatment for opioid overdose and opioid use disorder. J Exp Anal Behav. 2023 Mar;119(2):392-406. [Content Brief]
