Evidence map›Paper›PMID 24512267›Full record

ArticleJournal of medicinal chemistry2014

Design, synthesis, and structure-activity relationship of a novel series of GluN2C-selective potentiators.

Sommer S Zimmerman, Alpa Khatri, Ethel C Garnier-Amblard, Praseeda Mullasseril, Natalie L Kurtkaya, Stefka Gyoneva, Kasper B Hansen, Stephen F Traynelis, Dennis C Liotta

Erratum issuedOpen access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 24 papers.

0numbers the graph read from it
0cells of the map it votes in
24citing papers in PubMed
2.8field-weighted citation impact, top 10% 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

24 citing papers in PubMed, 45 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Modular Synthesis of trans-AChemistry (Weinheim an der Bergstrasse, Germany) · 2021
    Article
  6. Article
  7. New luciferin-based probe substrates for human CYP26A1.Biochemistry and biophysics reports · 2020
    Article
  8. Article
  9. Discovery of Dihydropyrrolo[1,2-Journal of medicinal chemistry · 2020
    Article
  10. Article
  11. Review
  12. Article
  13. Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. NMDA Receptors in the Central Nervous System.Methods in molecular biology (Clifton, N.J.) · 2017
    Article
  19. Article
  20. Article
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

9 authors at 1 institution in 2 countries.

Sommer S ZimmermanDepartment of Chemistry, Emory University , 1515 Dickey Drive, Atlanta, Georgia 30322, United States.
Alpa Khatri
Ethel C Garnier-Amblard
Praseeda Mullasseril
Natalie L Kurtkaya
Stefka Gyoneva
Kasper B Hansen
Stephen F Traynelis
Dennis C Liotta
Emory University · US

Funding

Graduate and Postdoctoral Training in ToxicologyT32ES012870 · NIEHS · EMORY UNIVERSITY · PI Carmen Joseph Marsit · 2004 to 2026
$9.1M
Graduate Training in the Pharmacological StudiesT32GM008602 · NIGMS · EMORY UNIVERSITY · PI HALL, RANDY A. · 1996 to 2021
$5.1M
Mechanism of Action of Novel Subunit-Selective NMDA Receptor ModulatorsR01NS065371 · NINDS · EMORY UNIVERSITY · PI TRAYNELIS, STEPHEN F · 2009 to 2018
$3.4M
Optimization of small molecule probesR21MH094525 · NIMH · EMORY UNIVERSITY · PI TRAYNELIS, STEPHEN F · 2012 to 2013
$458k
Mechanism of action of novel GluN2C NMDA receptor potentiatorsF32NS078873 · NINDS · EMORY UNIVERSITY · PI KHATRI, ALPA · 2012 to 2013
$106k
NIEHS NIH HHS ES012870NIEHS NIH HHS T32 ES012870NIGMS NIH HHS T32 GM008602NIMH NIH HHS MH094525NIMH NIH HHS R21 MH094525NINDS NIH HHS F32 NS078873NINDS NIH HHS NS065371NINDS NIH HHS NS078873NINDS NIH HHS R01 NS065371
6 · The paper itself

Abstract

NMDA receptors are tetrameric complexes composed of GluN1 and GluN2A-D subunits that mediate a slow Ca(2+)-permeable component of excitatory synaptic transmission. NMDA receptors have been implicated in a wide range of neurological diseases and thus represent an important therapeutic target. We herein describe a novel series of pyrrolidinones that selectively potentiate only NMDA receptors that contain the GluN2C subunit. The most active analogues tested were over 100-fold selective for recombinant GluN2C-containing receptors over GluN2A/B/D-containing NMDA receptors as well as AMPA and kainate receptors. This series represents the first class of allosteric potentiators that are selective for diheteromeric GluN2C-containing NMDA receptors.

Indexed as

AnimalsChromatography, High Pressure LiquidComputational BiologyDrug DesignExcitatory Amino Acid AgonistsHigh-Throughput Screening AssaysHumansIndicators and ReagentsMagnetic Resonance SpectroscopyModels, MolecularMolecular ConformationOocytesPatch-Clamp TechniquesPyrrolidinonesPyruvatesReceptors, N-Methyl-D-AspartateExcitatory Amino Acid AgonistsIndicators and ReagentsNR2C NMDA receptorPyrrolidinonesPyruvatesReceptors, N-Methyl-D-Aspartate

Identifiers

PMID24512267
PMCPMC3983368
OpenAlexW2332332954

What OpenQuestion holds

Textmetadata
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.