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Nalmefene hydrochloride (CAS 58895-64-0)

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Alternate Names:
Nalmefene hydrochloride is also known as
Application:
Nalmefene hydrochloride is an opioid receptor antagonist
CAS Number:
58895-64-0
Molecular Weight:
375.89
Molecular Formula:
C21H25NO3•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Nalmefene hydrochloride has been reported to be an opioid receptor antagonist. The opioid family of G-protein-coupled receptors contains three types of opioids; μ opioid receptor (MOR), δ opioid receptor (DOR), and κ opioid receptor (KOR). Activating these receptors leads to the release of neurotransmitters such as dopamine, serotonin, and norepinephrine. Nalmefene hydrochloride has been studied for its various biological activities, including anti-inflammatory, anti-nociceptive, anticonvulsant, and neuroprotective effects.

References:

  1. Acute effects of nalmefene on LH, prolactin, and testosterone in male rhesus monkeys.  |  Mello, NK., et al. 2000. Pharmacol Biochem Behav. 66: 275-83. PMID: 10880679
  2. Synergistic effects of cannabinoid inverse agonist AM251 and opioid antagonist nalmefene on food intake in mice.  |  Chen, RZ., et al. 2004. Brain Res. 999: 227-30. PMID: 14759503
  3. Prolonged central mu-opioid receptor occupancy after single and repeated nalmefene dosing.  |  Ingman, K., et al. 2005. Neuropsychopharmacology. 30: 2245-53. PMID: 15956985
  4. The permeation of nalmefene hydrochloride across different regions of ovine nasal mucosa.  |  Du, G., et al. 2006. Chem Pharm Bull (Tokyo). 54: 1722-4. PMID: 17139110
  5. In vivo characterization of the opioid antagonist nalmefene in mice.  |  Osborn, MD., et al. 2010. Life Sci. 86: 624-30. PMID: 20159022
  6. Potent inhibition of alcohol self-administration in alcohol-preferring rats by a kappa -opioid receptor antagonist.  |  Cashman, JR. and Azar, MR. 2014. J Pharmacol Exp Ther. 350: 171-80. PMID: 24817033
  7. In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene.  |  Xie, X., et al. 2015. PLoS One. 10: e0125953. PMID: 25938514
  8. Fighting Fire with Fire: Development of Intranasal Nalmefene to Treat Synthetic Opioid Overdose.  |  Krieter, P., et al. 2019. J Pharmacol Exp Ther. 371: 409-415. PMID: 30940694
  9. Clinically utilized kappa-opioid receptor agonist nalfurafine combined with low-dose naltrexone prevents alcohol relapse-like drinking in male and female mice.  |  Zhou, Y. and Kreek, MJ. 2019. Brain Res. 1724: 146410. PMID: 31469985
  10. Effects of nalmefene hydrochloride on TLR4 signaling pathway in rats with lung ischemia-reperfusion injury.  |  Zhang, NL., et al. 2020. Eur Rev Med Pharmacol Sci. 24: 461-468. PMID: 31957861
  11. Naloxone and nalmefene absorption delivered by hollow microneedles compared to intramuscular injection.  |  Papich, MG. and Narayan, RJ. 2022. Drug Deliv Transl Res. 12: 376-383. PMID: 34817831
  12. Effect of Different Absorption Enhancers on the Nasal Absorption of Nalmefene Hydrochloride.  |  Zhang, T., et al. 2022. AAPS PharmSciTech. 23: 143. PMID: 35578146
  13. Sufentanil combined with nalmefene reduce the adverse events in recovery period of patients undergoing uvulopalatopharyngoplasty - A randomized controlled trial.  |  Wang, J., et al. 2023. Heliyon. 9: e13241. PMID: 36755590
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