Evidence map›Paper›PMID 38810170›Full record

ArticleJournal of medicinal chemistry2024

Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression.

Loan Y Vu, Dan Luo, Kai Johnson, Emily D Denehy, Judy C Songrady, Jocelyn Martin, Riya Trivedi, Alexia R Alsum, Jakob D Shaykin, Chhabi Lal Chaudhary and 10 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

5 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

20 authors.

Loan Y VuDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Dan LuoDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Kai JohnsonDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Emily D DenehyDepartment of Psychology, University of Kentucky, Lexington, Kentucky 40536, United States.
Judy C SongradyDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Jocelyn MartinDepartment of Psychology, University of Kentucky, Lexington, Kentucky 40536, United States.
Riya TrivediDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Alexia R AlsumDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Jakob D ShaykinDepartment of Psychology, University of Kentucky, Lexington, Kentucky 40536, United States.
Chhabi Lal ChaudharyDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Eric J WoloshinDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Lindsay KornbergerDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Nazmul BhuiyanDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Sean ParkinDepartment of Chemistry, University of Kentucky, Lexington, Kentucky 40506, United States.
Qianru JiangCenter for Clinical Pharmacology, University of Health Sciences and Pharmacy and Washington University School of Medicine, St. Louis, Missouri 63110, United States.
Tao CheCenter for Clinical Pharmacology, University of Health Sciences and Pharmacy and Washington University School of Medicine, St. Louis, Missouri 63110, United States.
Warren AlilainSpinal Cord and Brain Injury Research Center (SCoBIRC), College of Medicine, University of Kentucky, Lexington, Kentucky 40536, United States.
Jill R TurnerDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.
Michael T BardoDepartment of Psychology, University of Kentucky, Lexington, Kentucky 40536, United States.
Thomas E PrisinzanoDepartment of Pharmaceutical Sciences, University of Kentucky, Lexington, Kentucky 40506, United States.

Funding

Kentucky Center for Clinical and Translational ScienceUL1TR001998 · NCATS · UNIVERSITY OF KENTUCKY · PI HARTMANN, KATHERINE E, KERN, PHILIP A · 2016 to 2025
$34.2M
Understanding the role of anti-apolipoprotein A-I antibodies in atherosclerotic cardiovascular diseaseP20GM130456 · NIGMS · UNIVERSITY OF KENTUCKY · PI M. Ashfaqul Alam · 2020 to 2026
$18.7M
Bruker AVANCE NEO 600 MHz High-Performance Digital NMR SpectrometerS10OD028690 · OD · UNIVERSITY OF KENTUCKY · PI GARNEAU-TSODIKOVA, SYLVIE · 2020 to 2020
$1.4M
Development of Agents for Synthetic Opioid OverdoseU01DA051377 · NIDA · UNIVERSITY OF KENTUCKY · PI PRISINZANO, THOMAS EDWARD · 2021 to 2023
$1.4M
NCATS NIH HHS UL1 TR001998NIDA NIH HHS U01 DA051377NIGMS NIH HHS P20 GM130456NIH HHS S10 OD028690
6 · The paper itself

Abstract

While in the process of designing more effective synthetic opioid rescue agents, we serendipitously identified a new chemotype of potent synthetic opioid. Here, we report that conformational constraint of a piperazine ring converts a mu opioid receptor (MOR) antagonist into a potent MOR agonist. The prototype of the series, which we have termed atoxifent (

Indexed as

Analgesics, OpioidFentanylReceptors, Opioid, muRespiratory InsufficiencyAnimalsBrainHumansMaleMiceNaltrexonePiperazinesRatsRats, Sprague-DawleyStructure-Activity RelationshipTissue DistributionAnalgesics, OpioidFentanylNaltrexonePiperazinesReceptors, Opioid, mu

Identifiers

PMID38810170
PMCPMC12054644

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

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.