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[1][2][3].

Product Specifications

CAS Number

[117339-76-1]

Product Name Alternative

M-CAM

UNSPSC

12352005

Target

Opioid Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

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

Molecular Formula

C30H32N2O4

Molecular Weight

484.59

References & Citations

[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.|[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. |[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.