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The Intriguing Effects of Substituents in the <i>N</i>-Phenethyl Moiety of Norhydromorphone: A Bifunctional Opioid from a Set of "Tail Wags Dog" Experiments.
Author: AdlerMartin W, BergmanJack, ChadderdonAaron M, CrowleyRachel Saylor, GellerEllen B, HannaRamsey D, HassanSergio A, HerdmanChristine A, InanSaadet, IrvinThomas C, JacobsonArthur E, KaskaSophia, KatzJonathan L, KopajticTheresa A, LeeYong-Sok, ParonisCarol A, PrisinzanoThomas E, RiceKenner C, TraynorJohn R, WangMeining, WitheySarah L
Original Abstract of the Article :
(-)-<i>N</i>-Phenethyl analogs of optically pure <i>N</i>-norhydromorphone were synthesized and pharmacologically evaluated in several in vitro assays (opioid receptor binding, stimulation of [<sup>35</sup>S]GTPγS binding, forskolin-induced cAMP accumulation assay, and MOR-mediated β-arres...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。
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* 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://www.ncbi.nlm.nih.gov/pmc/articles/PMC7321161/
データ提供:米国国立医学図書館(NLM)
Unlocking the Potential of Bifunctional Opioids
In the field of [pharmacology], [opioid research] continues to evolve, seeking new approaches to pain management while minimizing adverse effects. This research investigates the potential of [bifunctional opioids], specifically exploring the impact of substituents on the [N-phenethyl moiety] of norhydromorphone. The study employs a combination of [synthetic chemistry and pharmacological assays] to evaluate the structure-activity relationships of these compounds, offering valuable insights into the design of novel opioid analgesics.
A Novel Approach to Opioid Design
The study reveals the potential of [bifunctional opioids] that target both [mu-opioid receptors] (MOR) and [delta-opioid receptors] (DOR) as a promising approach to pain management. The researchers identified a specific compound, [N-p-chloro-phenethynorhydromorphone], that demonstrates [potent partial agonism at MOR and full agonism at DOR], suggesting a potential for reduced side effects compared to traditional MOR agonists. The study's findings pave the way for the development of new opioid analgesics with a more favorable therapeutic profile.
Exploring the Potential of Bifunctional Opioids
This research highlights the potential of [bifunctional opioids] in addressing the challenges associated with traditional opioid analgesics. The study's findings suggest that these novel compounds may offer a better balance between [efficacy and safety], potentially leading to improved pain management with fewer adverse effects. Further research is needed to fully explore the clinical potential of these promising compounds, but this research provides a compelling foundation for future investigations.
Dr.Camel's Conclusion
Opioid research, like a camel's journey through the desert, requires constant exploration and innovation. This research sheds light on the potential of bifunctional opioids, offering a new path towards more effective and safer pain management. Just as a camel adapts to its environment, we must continue to adapt and evolve our approaches to opioid therapy.
Date :
- Date Completed 2021-02-12
- Date Revised 2022-03-26
Further Info :
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