Methylation Products of 6β- N-Heterocyclic Substituted Naltrexamine Derivatives as Potential Peripheral Opioid Receptor Modulators.

Author: AkbaraliHamid I, DeweyWilliam L, KomlaEssie, ObengSamuel, SelleyDana E, StevensDavid L, WangHuiqun, ZhangYan, ZhengYi

Paper Details 
Original Abstract of the Article :
Two 6β- N-heterocyclic naltrexamine derivatives, NAP and NMP, have been identified as peripherally selective mu opioid receptor (MOR) antagonists. To further enhance the peripheral selectivity of both compounds, the 17-amino group and the nitrogen atom of the pyridine ring in both NAP and NMP were m...See full text at original site
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引用元:
https://pubmed.ncbi.nlm.nih.gov/30001114

データ提供:米国国立医学図書館(NLM)

Tailoring Naltrexamine Derivatives for Peripheral Opioid Receptor Modulation

Opioid receptors play a critical role in regulating pain perception, but their activation in the central nervous system can lead to adverse effects. This study explores the development of novel naltrexamine derivatives that selectively target peripheral opioid receptors, minimizing central nervous system side effects. The authors modified two naltrexamine derivatives, NAP and NMP, by methylation, creating dMNAP and dMNMP. They found that these modifications shifted the binding affinity to both mu and kappa opioid receptors, potentially enhancing peripheral selectivity. The results suggest that these compounds could offer a targeted approach to modulating opioid receptors, potentially leading to safer and more effective treatment options for peripheral conditions.

Navigating the Desert of Opioid Research: A Targeted Approach

This study showcases the innovative approach of tailoring naltrexamine derivatives for peripheral opioid receptor modulation. It's like a camel caravan navigating the desert, seeking a specific oasis to deliver its precious cargo. By modifying the original compounds, the authors have created new molecules that could potentially offer targeted relief for peripheral pain and other conditions, minimizing the risks associated with central nervous system activation.

Opioid Treatment: Balancing Benefits and Risks

Opioids are powerful medications that can provide significant pain relief, but they can also carry significant risks. This study highlights the importance of developing targeted approaches to opioid treatment, minimizing central nervous system side effects and maximizing the benefits for patients. It's a reminder to be mindful of the potential risks and benefits of opioid medications and to work closely with healthcare professionals to manage pain effectively and safely.

Dr.Camel's Conclusion

This research journey into the desert of opioid research reveals the potential of targeted approaches to pain management. By modifying existing compounds and carefully tailoring their effects, we can create new avenues for pain relief, minimizing the risks associated with traditional opioid medications. This study offers a ray of hope in the quest for safer and more effective treatments for pain, reminding us that innovation can often lead to breakthroughs in the most unexpected places.

Date :
  1. Date Completed 2019-12-23
  2. Date Revised 2020-03-06
Further Info :

Pubmed ID

30001114

DOI: Digital Object Identifier

NIHMS989182

Related Literature

SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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