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Comparison of the -opioid receptor antagonists methocinnamox (MCAM) and naloxone to reverse and prevent the ventilatory depressant effects of fentanyl, carfentanil, 3-methylfentanyl, and heroin in male rats.
Hiranita T, Ho NP, France CP. Hiranita T, et al. J Pharmacol Exp Ther. 2024 Feb 26:JPET-AR-2023-002032. doi: 10.1124/jpet.123.002032. Online ahead of print. J Pharmacol Exp Ther. 2024. PMID: 38409115 Free article.
The life-threatening effect of opioids is hypoventilation that can be reversed by the -opioid receptor (MOR) antagonist naloxone; however, because of the very short duration of action of naloxone, re-emergence of MOR agonist-induced hypoventilation can occur, requiring additional …
The life-threatening effect of opioids is hypoventilation that can be reversed by the -opioid receptor (MOR) antagonist naloxone; however, b …
Daily methocinnamox treatment dose-dependently attenuates fentanyl self-administration in rhesus monkeys.
Maguire DR, France CP. Maguire DR, et al. Neuropharmacology. 2024 Feb 1;243:109777. doi: 10.1016/j.neuropharm.2023.109777. Epub 2023 Nov 8. Neuropharmacology. 2024. PMID: 37944894
Opioid use disorder and opioid overdose continue to be significant public health challenges despite the availability of effective treatments. Methocinnamox (MCAM) is a novel, long-acting opioid receptor antagonist that might be an effective treatment for opioid use disorde …
Opioid use disorder and opioid overdose continue to be significant public health challenges despite the availability of effective treatments …
Behavioral pharmacology of methocinnamox: A potential new treatment for opioid overdose and opioid use disorder.
Maguire DR, France CP. Maguire DR, et al. J Exp Anal Behav. 2023 Mar;119(2):392-406. doi: 10.1002/jeab.831. Epub 2023 Feb 9. J Exp Anal Behav. 2023. PMID: 36759567 Free PMC article.
Studies in rodents and nonhuman primates demonstrate that methocinnamox prevents and reverses opioid-induced ventilatory depression and selectively blocks opioid self-administration. This work, taken together with rigorous in vitro and ex vivo studies investigating meth …
Studies in rodents and nonhuman primates demonstrate that methocinnamox prevents and reverses opioid-induced ventilatory depression a …
Attenuation of the Positive-Reinforcing Effects of Ultra-Potent Fentanyl Analogs, Along with Those of Fentanyl and Heroin, During Daily Treatment with Methocinnamox in Rhesus Monkeys.
Gerak LR, France CP. Gerak LR, et al. J Pharmacol Exp Ther. 2023 Mar;384(3):363-371. doi: 10.1124/jpet.122.001267. Epub 2022 Dec 27. J Pharmacol Exp Ther. 2023. PMID: 36575032 Free PMC article.
One drug under development is the opioid receptor antagonist methocinnamox (MCAM), which appears to offer advantages over currently available medications; however, some questions remain about its potential utility, including its ability to block the effects of ultra-potent …
One drug under development is the opioid receptor antagonist methocinnamox (MCAM), which appears to offer advantages over currently a …
The Potential of Methocinnamox as a Future Treatment for Opioid Use Disorder: A Narrative Review.
Jordan CG, Kennalley AL, Roberts AL, Nemes KM, Dolma T, Piper BJ. Jordan CG, et al. Pharmacy (Basel). 2022 Apr 19;10(3):48. doi: 10.3390/pharmacy10030048. Pharmacy (Basel). 2022. PMID: 35645327 Free PMC article. Review.
The opioid epidemic is an ongoing public health crisis, and the United States health system is overwhelmed with increasing numbers of opioid-related overdoses. Methocinnamox (MCAM) is a novel mu opioid receptor antagonist with an extended duration of action. ...
The opioid epidemic is an ongoing public health crisis, and the United States health system is overwhelmed with increasing numbers of opioid …
Effects of Daily Methocinnamox Treatment on Fentanyl Self-Administration in Rhesus Monkeys.
Maguire DR, France CP. Maguire DR, et al. J Pharmacol Exp Ther. 2022 Aug;382(2):181-187. doi: 10.1124/jpet.122.001233. Epub 2022 May 28. J Pharmacol Exp Ther. 2022. PMID: 35643857 Free PMC article.
Methocinnamox (MCAM), a long-acting mu-opioid receptor antagonist, attenuates the positive reinforcing effects of opioids, such as heroin and fentanyl, suggesting it could be an effective treatment of opioid use disorder (OUD). ...SIGNIFICANCE STATEMENT: Opioid use disorde …
Methocinnamox (MCAM), a long-acting mu-opioid receptor antagonist, attenuates the positive reinforcing effects of opioids, such as he …
Long-term antagonism and allosteric regulation of mu opioid receptors by the novel ligand, methocinnamox.
Zamora JC, Smith HR, Jennings EM, Chavera TS, Kotipalli V, Jay A, Husbands SM, Disney A, Berg KA, Clarke WP. Zamora JC, et al. Pharmacol Res Perspect. 2021 Dec;9(6):e00887. doi: 10.1002/prp2.887. Pharmacol Res Perspect. 2021. PMID: 34713624 Free PMC article.
In such circumstances, a long-lasting, non-surmountable antagonist would offer an improvement in overdose treatment. Methocinnamox (MCAM) has been reported to have a long duration of antagonist action at mu opioid receptors in vivo. ...
In such circumstances, a long-lasting, non-surmountable antagonist would offer an improvement in overdose treatment. Methocinnamox (M …
Methocinnamox Reverses and Prevents Fentanyl-Induced Ventilatory Depression in Rats.
Jimenez VM Jr, Castaneda G, France CP. Jimenez VM Jr, et al. J Pharmacol Exp Ther. 2021 Apr;377(1):29-38. doi: 10.1124/jpet.120.000387. Epub 2021 Jan 11. J Pharmacol Exp Ther. 2021. PMID: 33431611 Free PMC article.
., Narcan) is used currently to treat overdose; however, a short duration of action limits its clinical utility. Methocinnamox (MCAM) is a long-lasting opioid receptor antagonist that may reverse and prevent the ventilatory-depressant effects of fentanyl. ...SIGNIFICANCE S …
., Narcan) is used currently to treat overdose; however, a short duration of action limits its clinical utility. Methocinnamox (MCAM) …
Countermeasures for Preventing and Treating Opioid Overdose.
France CP, Ahern GP, Averick S, Disney A, Enright HA, Esmaeli-Azad B, Federico A, Gerak LR, Husbands SM, Kolber B, Lau EY, Lao V, Maguire DR, Malfatti MA, Martinez G, Mayer BP, Pravetoni M, Sahibzada N, Skolnick P, Snyder EY, Tomycz N, Valdez CA, Zapf J. France CP, et al. Clin Pharmacol Ther. 2021 Mar;109(3):578-590. doi: 10.1002/cpt.2098. Epub 2020 Nov 29. Clin Pharmacol Ther. 2021. PMID: 33113208 Free PMC article. Review.
This paper provides an overview of several presentations at that meeting that discussed emerging new approaches for treating opioid overdose, including the following: (1) intranasal nalmefene, a competitive, reversible opioid receptor antagonist with a longer duration of action t …
This paper provides an overview of several presentations at that meeting that discussed emerging new approaches for treating opioid overdose …
Methocinnamox (MCAM) antagonizes the behavioral suppressant effects of morphine without impairing delayed matching-to-sample accuracy in rhesus monkeys.
Minervini V, Disney A, Husbands SM, France CP. Minervini V, et al. Psychopharmacology (Berl). 2020 Oct;237(10):3057-3065. doi: 10.1007/s00213-020-05592-y. Epub 2020 Aug 9. Psychopharmacology (Berl). 2020. PMID: 32772146 Free PMC article.
RATIONALE: Opioid abuse remains a serious public health problem. The pseudoirreversible mu opioid receptor antagonist methocinnamox (MCAM) might be useful for treating opioid abuse and overdose. ...
RATIONALE: Opioid abuse remains a serious public health problem. The pseudoirreversible mu opioid receptor antagonist methocinnamox ( …
18 results