ArticleJournal of biomedical science2021
Design, synthesis, and preliminary evaluation of a potential synthetic opioid rescue agent.
Article in Journal of biomedical science, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
15 citing papers in PubMed, 18 citations in OpenAlex.
- Does Kappa Agonism Improve Reversal of 'Tranq-Dope' Overdose? Evidence from a Rodent Model.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Narcotics through time: exploring historical origins, synthetic advances, and clinical progress.Future medicinal chemistry · 2025Review
- Searching for Synthetic Opioid Rescue Agents. 2: Identification of an Ultra-Potent Synthetic Opioid Rescue Agent.Journal of medicinal chemistry · 2025Article
- Transformation of a Potent C9-Substituted Phenylmorphan into MOR Partial Agonists with Improvement of Metabolic Stability: An In Vitro, In Vivo, and In Silico Study.ACS chemical neuroscience · 2025Article
- Recommended Opioid Receptor Tool Compounds: ComparativeACS pharmacology & translational science · 2025Article
- Targeting αEnvironmental toxicology and pharmacology · 2024Article
- Functional Activity of Enantiomeric Oximes and Diastereomeric Amines and Cyano Substituents at C9 in 3-Hydroxy-Molecules (Basel, Switzerland) · 2024Article
- Xylazine suppresses fentanyl consumption during self-administration and induces a unique sex-specific withdrawal syndrome that is not altered by naloxone in rats.Experimental and clinical psychopharmacology · 2024Article
- Fentanyl overdose: Temporal effects and prognostic factors in SKH1 mice.Basic & clinical pharmacology & toxicology · 2024Article
- Potent MOR Agonists from 2'-Hydroxy-5,9-dimethyl-Molecules (Basel, Switzerland) · 2023Article
- A MOR Antagonist with High Potency and Antagonist Efficacy among Diastereomeric C9-Alkyl-SubstitutedMolecules (Basel, Switzerland) · 2023Article
- Discovery of a Potent Highly Biased MOR Partial Agonist among Diastereomeric C9-Hydroxyalkyl-5-phenylmorphans.Molecules (Basel, Switzerland) · 2023Article
- Synthesis and Pharmacological Evaluation of Enantiopure N-Substituted Ortho-c Oxide-Bridged 5-Phenylmorphans.Molecules (Basel, Switzerland) · 2022Article
- A Journey through Diastereomeric Space: The Design, Synthesis, In Vitro and In Vivo Pharmacological Activity, and Molecular Modeling of Novel Potent Diastereomeric MOR Agonists and Antagonists.Molecules (Basel, Switzerland) · 2022Article
- Novel Synthetic Opioids (NSO) Use in Opioid Dependents Entering Detoxification Treatment.Frontiers in psychiatry · 2022Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundOne of the most prominent opioid analgesics in the United States is the high potency agonist fentanyl. It is used in the treatment of acute and chronic pain and as an anesthetic adjuvant. When used inappropriately, however, ingestion of just a few milligrams of fentanyl or other synthetic opioid can cause opioid-induced respiratory depression (OIRD), often leading to death. Currently, the treatment of choice for OIRD is the opioid receptor antagonist naloxone. Recent reports, however, suggest that higher doses or repeated dosing of naloxone (due to recurrence of respiratory depression) may be required to reverse fully fentanyl-induced respiratory depression, rendering this treatment inadequate. To combat this synthetic opioid overdose crisis, this research aims at identifying a novel opioid reversal agent with enhanced efficacy towards fentanyl and other synthetic opioids.
methodsA series of naltrexone analogues were characterized for their ability to antagonize the effects of fentanyl in vitro utilizing a modified forskolin-induced cAMP accumulation assay. Lead analogue 29 was chosen to undergo further PK studies, followed by in vivo pharmacological analysis to determine its ability to antagonize opioid-induced antinociception in the hot plate assay.
resultsA series of potent MOR antagonists were identified, including the highly potent analogue 29 (IC
conclusionsMethods have been developed that have utility to identify enhanced rescue agents for the treatment of OIRD. Analogue 29, possessing potent MOR antagonist activity in vitro and in vivo, provides a promising lead in our search for an enhanced synthetic opioid rescue agent.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.