Evidence map›Paper›PMID 41102225›Full record

ArticleScientific reports2025

Novel dual kappa/mu opioid ligands based on a tetrahydroisoquinoline-valine hybrid nucleus.

Ahmad Abdelwaly, Hesham Safwan, Shamba Chatterjee, Mohamed Elsayed, Khaled M Darwish, Amar Chittiboyina, Mohamed A Helal

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Scientific reports, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

7 authors.

Ahmad AbdelwalyBiomedical Sciences Program, University of Science and Technology, Zewail City of Science and Technology, Giza, 12587, Egypt.
Hesham SafwanBiomedical Sciences Program, University of Science and Technology, Zewail City of Science and Technology, Giza, 12587, Egypt.
Shamba ChatterjeeNational Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS, 38677, USA.
Mohamed ElsayedPharmacology Department, Faculty of Pharmacy, Suez Canal University, Ismailia, 41522, Egypt.
Khaled M DarwishMedicinal Chemistry Department, Faculty of Pharmacy, Galala University, Galala, Egypt.
Amar ChittiboyinaNational Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS, 38677, USA.
Mohamed A HelalBiomedical Sciences Program, University of Science and Technology, Zewail City of Science and Technology, Giza, 12587, Egypt. mhelal@zewailcity.edu.eg.

Funding

Science, Technology, and Innovation Funding Authority (STDF, Egypt) U.S. - Egypt Science and Technology Joint Fund, Grant #1086, Cycle 18
6 · The paper itself

Abstract

Opioid addiction constitutes a significant global health challenge. Kappa opioid receptor (KOP) modulators have demonstrated efficacy in treating resistant drug abuse cases. However, till date, no selective KOP antagonists have successfully reached the market. In this study, we employed structure-based design to modify JDTic, the most potent KOP antagonist, into a series of novel analogs based on a tetrahydroisoquinoline (THIQ)-valine hybrid scaffold. More than 20 compounds were synthesized and assessed for binding affinities to the three opioid receptor subtypes. Ten derivatives showed a binding Ki of less than 10 µM for KOP. Subsequent functional characterization using [

Indexed as

Receptors, Opioid, kappaReceptors, Opioid, muTetrahydroisoquinolinesValineAnalgesics, OpioidAnimalsHumansLigandsMaleMiceStructure-Activity RelationshipAnalgesics, OpioidLigandsReceptors, Opioid, kappaReceptors, Opioid, muTetrahydroisoquinolinesValineAddictionDockingIsoquinolinesKappa-isoformOpioid receptors

Identifiers

PMID41102225
PMCPMC12533025

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.