Evidence map›Paper›PMID 22735771›Full record

ArticleNeuropharmacology2013

Functional analysis of a novel positive allosteric modulator of AMPA receptors derived from a structure-based drug design strategy.

Jonathan E Harms, Morris Benveniste, John K F Maclean, Kathryn M Partin, Craig Jamieson

Open access · greenAbstract read
In one paragraph

Article in Neuropharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
1.4field-weighted citation impact, top 22% 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

16 citing papers in PubMed, 37 citations in OpenAlex.

  1. Review
  2. Article
  3. 5-Nitroisoxazoles inInternational journal of molecular sciences · 2023
    Article
  4. Review
  5. Article
  6. Article
  7. Article
  8. Article
  9. Article
  10. Article
  11. Novel bivalent positive allosteric modulators of AMPA receptor.Doklady. Biochemistry and biophysics · 2015
    Article
  12. Review
  13. Article
  14. Article
  15. Article
  16. Use of allosteric targets in the discovery of safer drugs.Medical principles and practice : international journal of the Kuwait University, Health Science Centre · 2013
    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

5 authors at 4 institutions in 2 countries.

Jonathan E HarmsDepartment of Biomedical Sciences, Colorado State University, Fort Collins, CO 80523-1617, USA. jonathan.harms@colostate.edu
Morris Benveniste
John K F Maclean
Kathryn M Partin
Craig Jamieson
Colorado State University · USInternational Union of Pure and Applied Chemistry · USMerck & Co., Inc., Rahway, NJ, USA (United States) · USMorehouse School of Medicine · US

Funding

GLUTAMATE RECEPTOR DESENSITIZATION AND ITS MODULATIONR01MH064700 · NIMH · COLORADO STATE UNIVERSITY-FORT COLLINS · PI PARTIN, KATHRYN MCKAY · 2001 to 2012
$2.4M
Influence of NMDA Receptors on EPSP Summation in Normal and Epileptic RatsS11NS055883 · NINDS · MOREHOUSE SCHOOL OF MEDICINE · PI BENVENISTE, MORRIS J. · 2007 to 2011
$1.2M
NIMH NIH HHS MH064700NIMH NIH HHS R01 MH064700NINDS NIH HHS S11 NS055883NINDS NIH HHS S11NS055883
6 · The paper itself

Abstract

Positive allosteric modulators of α-amino-3-hydroxy-5-methyl-isoxazole-propionic acid (AMPA) receptors facilitate synaptic plasticity and can improve various forms of learning and memory. These modulators show promise as therapeutic agents for the treatment of neurological disorders such as schizophrenia, ADHD, and mental depression. Three classes of positive modulator, the benzamides, the thiadiazides, and the biarylsulfonamides differentially occupy a solvent accessible binding pocket at the interface between the two subunits that form the AMPA receptor ligand-binding pocket. Here, we describe the electrophysiological properties of a new chemotype derived from a structure-based drug design strategy (SBDD), which makes similar receptor interactions compared to previously reported classes of modulator. This pyrazole amide derivative, JAMI1001A, with a promising developability profile, efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms. This article is part of a Special Issue entitled 'Cognitive Enhancers'.

Indexed as

AcetamidesAllosteric SiteBenzamidesChemistry, PharmaceuticalDatabases, ProteinDrug DesignExcitatory Amino Acid AgonistsHEK293 CellsHumansKidneyKineticsLigandsNootropic AgentsProtein ConformationProtein SubunitsPyrazoles2-(2-(4-(hydroxymethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetamido)-4,5,6,7 tetrahydrobenzo(b)thiophene-3-carboxamideAcetamidesBenzamidesExcitatory Amino Acid AgonistsLigandsNootropic AgentsProtein SubunitsPyrazolesReceptors, AMPARecombinant Fusion ProteinsSulfonamidesThiophenes

Identifiers

PMID22735771
PMCPMC3445766
OpenAlexW2058858473

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.