Evidence map›Paper›PMID 38971050›Full record

ArticleEuropean journal of medicinal chemistry2024

Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists.

Ashley E Trojniak, Vuong Q Dang, Kerri M Czekner, Robin J Russo, Lilyan M Mather, Edward L Stahl, Michael D Cameron, Laura M Bohn, Jeffrey Aubé

Abstract read
In one paragraph

Article in European 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 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing 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

7 citing papers in PubMed.

  1. Article
  2. Triazole 187 is a biased KOR agonist that suppresses itch without sedation and induces anxiolytic-like behaviors in mice.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026
    Article
  3. Article
  4. Review
  5. Article
  6. Review
  7. Article
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

9 authors.

Ashley E TrojniakDivision of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599-7363, USA.
Vuong Q DangThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, 130 Scripps Way, Jupiter, FL, 33458, USA.
Kerri M CzeknerThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, 130 Scripps Way, Jupiter, FL, 33458, USA; The Skaggs Graduate School of Chemical and Biological Sciences at Scripps Research, Jupiter, FL, 33458, USA.
Robin J RussoThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, 130 Scripps Way, Jupiter, FL, 33458, USA; The Skaggs Graduate School of Chemical and Biological Sciences at Scripps Research, Jupiter, FL, 33458, USA.
Lilyan M MatherDivision of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599-7363, USA.
Edward L StahlThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, 130 Scripps Way, Jupiter, FL, 33458, USA.
Michael D CameronThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, 130 Scripps Way, Jupiter, FL, 33458, USA.
Laura M BohnThe Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, 130 Scripps Way, Jupiter, FL, 33458, USA; The Skaggs Graduate School of Chemical and Biological Sciences at Scripps Research, Jupiter, FL, 33458, USA.
Jeffrey AubéDivision of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599-7363, USA. Electronic address: jaube@unc.edu.

Funding

Virology Research Program (Program 4)P30CA016086 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI Deborah F. Tate · 1985 to 2026
$201.5M
TO AWARD THE BASE PERIOD FOR NIMH PSYCHOACTIVE DRUG SCREENING PROGRAM (PDSP). BASE POP: 08/30/2023-08/29/2024.75N95023C00021 · NIDA · UNIV OF NORTH CAROLINA CHAPEL HILL · PI ROTH, BRYAN · 2023 to 2025
$9.0M
Novel Probes of the Kappa Opioid Receptor: Chemistry, Pharmacology, and BiologyR01DA031927 · NIDA · UNIVERSITY OF SOUTH FLORIDA · PI Jeffrey Aube, Laura M. Bohn · 2011 to 2026
$8.4M
Biased Kappa Opioid Agonists as Non-addictive AnalgesicsR01DA048490 · NIDA · WAKE FOREST UNIVERSITY HEALTH SCIENCES · PI JONES, SARA RAULERSON, MARTIN, THOMAS JEFFREY · 2019 to 2023
$3.4M
Request for a 500 MHz NMR console and nitrogen-cooled cryoprobeS10OD032476 · OD · UNIV OF NORTH CAROLINA CHAPEL HILL · PI LEE, ANDREW L · 2022 to 2022
$599k
NCI NIH HHS P30 CA016086NIDA NIH HHS 75N95023C00021NIDA NIH HHS R01 DA031927NIDA NIH HHS R01 DA048490NIH HHS S10 OD032476
6 · The paper itself

Abstract

Kappa opioid receptor (KOR) agonists represent promising therapeutics for pain relief due to their analgesic properties along with lower abuse potential than opioids that act at the mu opioid receptor. However, typical KOR agonists produce sedation and dysphoria. Previous studies have shown that G protein signaling-biased KOR agonists may present a means to untangle the desired analgesic properties from undesired side effects. In this paper, we report a new series of G protein signaling-biased KOR agonists entailing -S- → -CH

Indexed as

Receptors, Opioid, kappaTriazolesAnimalsDose-Response Relationship, DrugGTP-Binding ProteinsHumansMolecular StructureStructure-Activity RelationshipGTP-Binding ProteinsReceptors, Opioid, kappaTriazolesBiased agonistBioisostereKappa opioid receptorMicrosomal stabilityStructure–activity relationships

Identifiers

PMID38971050
PMCPMC11316643

What OpenQuestion holds

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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.