Evidence map›Paper›PMID 21216504›Full record

ArticleEuropean journal of medicinal chemistry2011

Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic.

Gianfranco Balboni, Severo Salvadori, Ewa D Marczak, Brian I Knapp, Jean M Bidlack, Lawrence H Lazarus, Xuemei Peng, Yu Gui Si, John L Neumeyer

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2011. 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
0.5field-weighted citation impact, top 44% 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

7 citing papers in PubMed, 14 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Article
  5. Article
  6. Review
  7. Heteromeric dopamine receptor signaling complexes: emerging neurobiology and disease relevance.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2014
    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

9 authors at 6 institutions in 2 countries.

Gianfranco BalboniDepartment of Toxicology, University of Cagliari, Via Ospedale 72, I-09124 Cagliari, Italy. gbalboni@unica.it
Severo Salvadori
Ewa D Marczak
Brian I Knapp
Jean M Bidlack
Lawrence H Lazarus
Xuemei Peng
Yu Gui Si
John L Neumeyer
McLean Hospital · USNational Institute of Environmental Health Sciences · USUniversity of Rochester · USHarvard University · USUniversity of Cagliari · ITUniversity of Ferrara · IT

Funding

Mixed Kappa/Mu Opioids: Synthesis and EvaluationR01DA014251 · NIDA · MC LEAN HOSPITAL (BELMONT, MA) · PI NEUMEYER, JOHN L · 2001 to 2012
$3.4M
OPIOID RECEPTORS ON LYMPHOCYTES AND BRAINK05DA000360 · NIDA · UNIVERSITY OF ROCHESTER · PI BIDLACK, JEAN M · 1998 to 2007
$893k
Bioactivity Of Opioidmimetic SubstancesZ01ES100472 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI LAZARUS, LAWRENCE H · 2002 to 2008
$572k
Opioid Peptides--Molecular Mechanism Of ActionZIAES090053 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI LAZARUS, LAWRENCE H · 2009 to 2010
$571k
Bioactivity Of Opioidmimetic SubstancesZIAES100472 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI LAZARUS, LAWRENCE H · 2009 to 2010
$571k
Intramural NIH HHS Z01 ES100472Intramural NIH HHS Z99 ES999999Intramural NIH HHS ZIA ES090053Intramural NIH HHS ZIA ES100472NIDA NIH HHS K05 DA000360NIDA NIH HHS K05-DA 00360NIDA NIH HHS R01 DA014251NIDA NIH HHS R01-DA14251
6 · The paper itself

Abstract

Bifunctional ligands containing an ester linkage between morphine and the δ-selective pharmacophore Dmt-Tic were synthesized, and their binding affinity and functional bioactivity at the μ, δ and κ opioid receptors determined. Bifunctional ligands containing or not a spacer of β-alanine between the two pharmacophores lose the μ agonism deriving from morphine becoming partial μ agonists 4 or μ antagonists 5. Partial κ agonism is evidenced only for compound 4. Finally, both compounds showed potent δ antagonism.

Indexed as

Narcotic AntagonistsAnimalsCHO CellsCricetinaeCricetulusDipeptidesEstersHumansLigandsMolecular ConformationMorphineStereoisomerismStructure-Activity RelationshipTetrahydroisoquinolines2',6'-dimethyltyrosyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acidDipeptidesEstersLigandsMorphineNarcotic AntagonistsTetrahydroisoquinolines

Identifiers

PMID21216504
PMCPMC3035428
OpenAlexW1980804234

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.