Evidence map›Paper›PMID 28002957›Full record

ArticleJournal of medicinal chemistry2016

Development of Radiolabeled Ligands Targeting the Glutamate Binding Site of the N-Methyl-d-aspartate Receptor as Potential Imaging Agents for Brain.

Lucia Tamborini, Ying Chen, Catherine A Foss, Andrea Pinto, Andrew G Horti, Stephen F Traynelis, Carlo De Micheli, Ronnie C Mease, Kasper B Hansen, Paola Conti and 1 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing 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

6 citing papers in PubMed.

  1. Discovery of GluN2A subtype-selectiveActa pharmaceutica Sinica. B · 2024
    Review
  2. Review
  3. Metal-free C-C bond formationChemical science · 2019
    Article
  4. Review
  5. Review
  6. Structural basis of subunit selectivity for competitive NMDA receptor antagonists with preference for GluN2A over GluN2B subunits.Proceedings of the National Academy of Sciences of the United States of America · 2017
    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

11 authors.

Lucia TamboriniDepartment of Pharmaceutical Sciences, Università degli Studi di Milano , Via Mangiagalli 25, 20133 Milano, Italy.
Ying ChenRussell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical School , Baltimore, Maryland 21287, United States.
Catherine A FossRussell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical School , Baltimore, Maryland 21287, United States.
Andrea PintoDepartment of Pharmaceutical Sciences, Università degli Studi di Milano , Via Mangiagalli 25, 20133 Milano, Italy.
Andrew G HortiRussell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical School , Baltimore, Maryland 21287, United States.
Stephen F TraynelisDepartment of Pharmacology, Emory University School of Medicine , Atlanta, Georgia 30322, United States.
Carlo De MicheliDepartment of Pharmaceutical Sciences, Università degli Studi di Milano , Via Mangiagalli 25, 20133 Milano, Italy.
Ronnie C MeaseRussell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical School , Baltimore, Maryland 21287, United States.
Kasper B HansenDepartment of Biomedical & Pharmaceutical Sciences, University of Montana , 32 Campus Drive, Missoula, Montana 59812, United States.
Paola ContiDepartment of Pharmaceutical Sciences, Università degli Studi di Milano , Via Mangiagalli 25, 20133 Milano, Italy.ORCID 0000-0003-2140-0567
Martin G PomperRussell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical School , Baltimore, Maryland 21287, United States.

Funding

Surveillance genome sequencing to detect SARS-CoV-2 virus variants in MontanaP20GM103546 · NIGMS · UNIVERSITY OF MONTANA · PI BOWLER, BRUCE E · 2012 to 2021
$19.2M
PSMA-based Cancer Imaging AgentsR01CA134675 · NCI · UT SOUTHWESTERN MEDICAL CENTER · PI POMPER, MARTIN G · 2009 to 2025
$6.2M
Mechanism of Action of Novel Subunit-Selective NMDA Receptor ModulatorsR01NS065371 · NINDS · EMORY UNIVERSITY · PI TRAYNELIS, STEPHEN F · 2009 to 2018
$3.4M
Structural and functional investigation of negative allosteric NMDA receptor modulationR01NS097536 · NINDS · UNIVERSITY OF MONTANA · PI Kasper Boe Hansen · 2016 to 2026
$3.4M
NCI NIH HHS R01 CA134675NIGMS NIH HHS P20 GM103546NINDS NIH HHS R01 NS065371NINDS NIH HHS R01 NS097536
6 · The paper itself

Abstract

Abnormal activity of various N-methyl-d-aspartate receptor (NMDAR) subtypes has been implicated in a wide variety of neurological disorders such as Alzheimer's disease, schizophrenia, and epilepsy. Imaging agents for PET and SPECT that target NMDARs in a subtype-selective fashion may enable better characterization of those disorders and enhance drug development. On the basis of a pyrazoline derivative that demonstrated neuroprotective effects in vivo, we synthesized a series of para-substituted analogues and measured their affinities to various NMDAR subtypes. Compounds 4a-c and 4e showed greater, nanomolar affinity for the GluN1/2A subtype versus GluN1/2B. Dicarbomethoxy (pro-drug) analogues of [

Indexed as

AnimalsBinding SitesBrainCarbon RadioisotopesDose-Response Relationship, DrugGlutamic AcidIodine RadioisotopesLigandsMaleMiceMice, NudeMolecular StructureNeuroprotective AgentsPositron Emission Tomography Computed TomographyPyrazolesReceptors, N-Methyl-D-AspartateCarbon RadioisotopesGlutamic AcidIodine RadioisotopesLigandsNeuroprotective AgentsPyrazolesReceptors, N-Methyl-D-Aspartate

Identifiers

PMID28002957
PMCPMC5484777

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.