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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- CAS No.: 117339-76-1
- Formule: C30H32N2O4
- Masse moléculaire:484.59
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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μ Opioid Receptor/MOR 0.6 nM (Ki) |
κ Opioid Receptor/KOR 4.9 nM (Ki) |
δ Opioid Receptor/DOR 2.2 nM (Ki) |
Methocinnamox binds very tightly to the μ receptor in the mouse brain tissue and has an extremely slow dissociation rate, but it has no effect on the binding sites of the δ and κ receptors[3].
Methocinnamox insurmountable and pseudoirreversible blocks the inhibitory effects of DAMGO (HY-P0210), psychoactive compound and morphine on the accumulation of cAMP in HEK293 cells that have been transfected with human μ-opioid receptor[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Methocinnamox (0.0001-10 mg/kg, i.v. or 10 mg/kg, i.v. and s.c, single dose) effectively reverses and protects the respiratory depression caused by psychoactive compound in rats[2].
Methocinnamox (0.32 mg/kg, s.c., single dose, or once every 12 days for 5 doses; 0.032 mg/kg, once daily for 21 days) reduces the self-administration behavior of opioids, but it has no effect on the self-administration of the response to food in rhesus monkeys[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Paw inflammation and mechanical sensitivity, gastrointestinal transit and physical dependence and withdrawal model established in male Sprague-Dawley rats[1]
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Dosage:10 mg/kg
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Administration:Subcutaneous injection (s.c.), single dose
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Result:Significantly reduced the analgesic effect of morphine on paw inflammation and this antagonistic effect persisted for at least 15 days.
Blocked the increase in body temperature caused by morphine, with the effect lasting for more than 15 days.
Completely blocked the inhibitory effect of morphine on gastrointestinal peristalsis until 21 days.
Did not result in a longer or more severe withdrawal syndrome.
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Animal Model:Reversal of psychoactive compound assay established in adult male Sprague-Dawley rats[2]
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Dosage:0.0001, 0.001, 0.01, 0.1, 1, 10 mg/kg (i.v.) and 10 mg/kg (i.v.) and (s.c)
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Administration:Intravenous injection (i.v.) and subcutaneous injection (s.c.), single dose
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Result:Dose-dependently rapidly reversed severe respiratory depression.
Provide long-lasting protection and effectively prevent the "re-anesthesia" phenomenon that occurs after rescue.
Exhibited a significantly longer duration of action when administered subcutaneously (s.c.) compared to intravenous (i.v.) administration at the same dose.
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Animal Model:Self-Administration model established in rhesus monkeys[3]
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Dosage:0.032 mg/kg and 0.32 mg/kg
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Administration:Subcutaneous injection (s.c.), single dose, or once every 12 days for 5 doses (0.32 mg/kg); once daily for 21 days (0.032 mg/kg)
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Result:Effectively and selectively blocked the reinforcing effects (euphoria) of opioid agent.
Reduced the relative reinforcing value of opioid drugs, making non-drug rewards (such as food) more attractive.
Did not impair advanced cognitive functions such as working memory or attention.
had no significant effect on the cardiovascular system and body temperature regulation at 3.2 mg/kg.
Chemical Information
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CAS No. 117339-76-1
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Masse moléculaire 484.59
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Formule C30H32N2O4
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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
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Synonyms
M-CAM
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Methocinnamox Related Classifications
HY-135698 Related Classifications
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