Evidence map›Paper›PMID 20137938›Full record

ArticleBioorganic & medicinal chemistry letters2010

Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.

Steven Ballet, Ewa D Marczak, Debby Feytens, Severo Salvadori, Yusuke Sasaki, Andrew D Abell, Lawrence H Lazarus, Gianfranco Balboni, Dirk Tourwé

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. 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.

Steven BalletDepartment of Organic Chemistry, Vrije Universiteit Brussel, B-1050 Brussels, Belgium. sballet@vub.ac.be
Ewa D Marczak
Debby Feytens
Severo Salvadori
Yusuke Sasaki
Andrew D Abell
Lawrence H Lazarus
Gianfranco Balboni
Dirk Tourwé

Funding

Opioid Peptides--Molecular Mechanism Of ActionZ01ES090053 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI LAZARUS, LAWRENCE H · 1988 to 2008
$572k
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 ES090053Intramural NIH HHS Z01 ES100472Intramural NIH HHS Z99 ES999999
6 · The paper itself

Abstract

The dimerization and trimerization of the Dmt-Tic, Dmt-Aia and Dmt-Aba pharmacophores provided multiple ligands which were evaluated in vitro for opioid receptor binding and functional activity. Whereas the Tic- and Aba multimers proved to be dual and balanced delta/mu antagonists, as determined by the functional [S(35)]GTPgammaS binding assay, the dimerization of potent Aia-based 'parent' ligands unexpectedly resulted in substantial less efficient receptor binding and non-active dimeric compounds.

Indexed as

LigandsAnimalsBenzazepinesDimerizationDrug DesignIndolesProtein BindingRatsReceptors, Opioid, deltaReceptors, Opioid, muTetrahydroisoquinolinesBenzazepinesIndolesLigandsReceptors, Opioid, deltaReceptors, Opioid, muTetrahydroisoquinolines

Identifiers

PMID20137938
PMCPMC2840614

What OpenQuestion holds

Textmetadata
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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.