Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].

Author: AnanthanSubramaniam, BartlettJeffrey L, BilskyEdward J, DavisPeg, DerschChristina M, KhareNaveen K, PorrecaFrank, RothmanRichard B, SainiSurendra K, SeitzLainne E

Paper Details 
Original Abstract of the Article :
A series of pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone (7a-k) were synthesized and evaluated for binding affinity at the opioid delta, micro, and kappa receptors in brain membranes using radioligand binding assays and for functional activity in vitro using [(35)S]GTP-gamm...See full text at original site
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引用元:
https://doi.org/10.1021/jm030311v

データ提供:米国国立医学図書館(NLM)

Identifying Opioid Ligands with Mixed Agonist/Antagonist Activity

This research delves into the intricate world of [opioid receptors] and their potential as targets for novel pain relief strategies. The authors meticulously synthesized and tested a series of [pyridomorphinans] derived from known opioid compounds. Their investigation led to the identification of [ligands with mixed micro agonist/delta antagonist activity], a promising avenue for developing new analgesic drugs. This discovery is particularly noteworthy because [these ligands could potentially overcome the limitations of existing opioid therapies], such as tolerance and dependence.

Unlocking the Potential of Mixed Agonist/Antagonist Ligands

The results of this study offer a glimpse into the future of pain management. These [mixed micro agonist/delta antagonist ligands] could pave the way for [novel analgesic drugs with improved safety profiles], potentially transforming the lives of individuals suffering from chronic pain.

A Promising Path to Pain Relief

The discovery of these novel opioid ligands holds great promise for alleviating pain without the debilitating side effects of traditional opioids. This research, like a cool spring in the scorching desert, provides a glimmer of hope for those seeking effective pain relief.

Dr.Camel's Conclusion

This research unveils the intricate dance of opioid receptors, demonstrating the potential of carefully crafted molecules to alleviate pain without the pitfalls of traditional opioids. It's like finding a hidden oasis in the vast desert of pain management, offering a new path to relief and a brighter future for those seeking solace from suffering.
Date :
  1. Date Completed 2004-04-23
  2. Date Revised 2014-11-20
Further Info :

Pubmed ID

14998329

DOI: Digital Object Identifier

10.1021/jm030311v

Related Literature

SNS
PICO Info
in preparation
Languages

English

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