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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
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
Dr.Camel's Paper Summary Blogラクダ博士について
ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
難解な医学論文を、専門知識のない方にも理解しやすいように、噛み砕いて説明することを目指しています。
* ラクダ博士による解説は、あくまで論文の要点をまとめたものであり、原論文の完全な代替となるものではありません。詳細な内容については、必ず原論文をご参照ください。
* ラクダ博士は架空のキャラクターであり、実際の医学研究者や医療従事者とは一切関係がありません。
* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。
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 :
- Date Completed 2019-12-23
- Date Revised 2020-03-06
Further Info :
Related Literature
English
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