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

Paper Details 
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]GTP&#947;S binding, forskolin-induced cAMP accumulation assay, and MOR-mediated &#946;-arres...See full text at original site
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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 :
  1. Date Completed 2021-02-12
  2. Date Revised 2022-03-26
Further Info :

Pubmed ID

32517185

DOI: Digital Object Identifier

PMC7321161

Related Literature

SNS
PICO Info
in preparation
Languages

English

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