Evidence map›Paper›PMID 25703306›Full record

ArticleBioorganic & medicinal chemistry2015

Design, synthesis, and biological evaluation of a series of bifunctional ligands of opioids/SSRIs.

Mehr-un-Nisa, Munawar A Munawar, Yeon Sun Lee, David Rankin, Jawaria Munir, Josephine Lai, Misbahul A Khan, Victor J Hruby

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2015. 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
0.3field-weighted citation impact, top 47% of its field
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, 4 citations in OpenAlex.

  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

8 authors at 3 institutions in 2 countries.

Mehr-un-NisaInstitute of Chemistry, University of the Punjab, Lahore 54590, Pakistan; Department of Chemistry and Biochemistry, University of Arizona, Tucson, AZ 85721, USA.
Munawar A MunawarInstitute of Chemistry, University of the Punjab, Lahore 54590, Pakistan.
Yeon Sun LeeDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ 85721, USA. Electronic address: yeon@email.arizona.edu.
David RankinDepartment of Pharmacology, University of Arizona, Tucson, AZ 85721, USA.
Jawaria MunirInstitute of Chemistry, University of the Punjab, Lahore 54590, Pakistan; Institute of Molecular Sciences & Bioinformatics, Lahore 54000, Pakistan.
Josephine LaiDepartment of Pharmacology, University of Arizona, Tucson, AZ 85721, USA.
Misbahul A KhanInstitute of Chemistry, University of the Punjab, Lahore 54590, Pakistan.
Victor J HrubyDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ 85721, USA. Electronic address: hruby@email.arizona.edu.
University of Arizona · USUniversity of the Punjab · PKInstitute of Molecular Sciences and Bioinformatics · PK

Funding

THERAPEUTIC PROFILES OF OPIOID DELTA RECEPTORS--NEW MODALITIESP01DA006284 · NIDA · UNIVERSITY OF ARIZONA · PI HRUBY, VICTOR J · 1989 to 2015
$14.8M
NOVEL NON-PEPTIDE OPIOID LIGANDS FOR PAINR01DA013449 · NIDA · UNIVERSITY OF ARIZONA · PI HRUBY, VICTOR J · 2000 to 2015
$6.8M
NIDA NIH HHS P01 DA006284NIDA NIH HHS P01DA006284NIDA NIH HHS R01 DA013449NIDA NIH HHS R01DA013449
6 · The paper itself

Abstract

A series of opioid and serotonin re-uptake inhibitors (SSRIs) bifunctional ligands have been designed, synthesized, and tested for their activities and efficacies at μ-, δ- and κ opioid receptors and SSRIs receptors. Most of the compounds showed high affinities for μ- and δ-opioid receptors and lower affinities for SSRIs and κ opioid receptors. A docking study on the μ-opioid receptor binding pocket has been carried out for ligands 3-11. The ligands 7 and 11 have displayed the highest binding profiles for the μ-opioid receptor binding site with ΔGbind (-12.14kcal/mol) and Ki value (1.0nM), and ΔGbind (-12.41kcal/mol) and Ki value (0.4nM), respectively. Ligand 3 was shown to have the potential of dual acting serotonin/norepinephrine re-uptake inhibitor (SNRI) antidepressant activity in addition to opioid activities, and thus could be used for the design of multifunctional ligands in the area of a novel approach for the treatment of pain and depression.

Indexed as

Drug DesignDose-Response Relationship, DrugHumansLigandsMolecular StructureReceptors, OpioidReceptors, SerotoninSelective Serotonin Reuptake InhibitorsStructure-Activity RelationshipLigandsReceptors, OpioidReceptors, SerotoninSelective Serotonin Reuptake InhibitorsBifunctional ligandsDepressionOpioidPainSSRIsSynergistic effect

Identifiers

PMID25703306
PMCPMC4349363
OpenAlexW2069903714

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.