Evidence map›Paper›PMID 27639297›Full record

ArticleEuropean journal of pharmacology2016

Ester to amide substitution improves selectivity, efficacy and kinetic behavior of a benzodiazepine positive modulator of GABA

Tamara Timić Stamenić, Michael M Poe, Sabah Rehman, Anja Santrač, Branka Divović, Petra Scholze, Margot Ernst, James M Cook, Miroslav M Savić

Open access · bronzeAbstract read
In one paragraph

Article in European journal of pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
2.0field-weighted citation impact, top 15% 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

20 citing papers in PubMed, 35 citations in OpenAlex.

  1. Article
  2. Enantiomer-specific modulation of GABAPsychopharmacology · 2026
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  9. Hippocampal α5-GABABiological psychiatry global open science · 2023
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  10. Effects of α5 GABACNS neuroscience & therapeutics · 2022
    Article
  11. Symptomatic and neurotrophic effects of GABAA receptor positive allosteric modulation in a mouse model of chronic stress.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2022
    Article
  12. Article
  13. Article
  14. Article
  15. Article
  16. Article
  17. Positive modulation of α5 GABAInternational journal of developmental neuroscience : the official journal of the International Society for Developmental Neuroscience · 2017
    Article
  18. Neurobiological correlates of state-dependent context fear.Learning & memory (Cold Spring Harbor, N.Y.) · 2017
    Article
  19. Article
  20. 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 3 institutions in 3 countries.

Tamara Timić StamenićDepartment of Pharmacology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Michael M PoeDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, P.O. Box 413, Milwaukee, Wisconsin 53201, USA.
Sabah RehmanDepartment of Molecular Neurosciences, Center for Brain Research, Medical University of Vienna, Vienna, Austria.
Anja SantračDepartment of Pharmacology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Branka DivovićDepartment of Pharmacology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Petra ScholzeDepartment of Pathobiology of the Nervous System, Center for Brain Research, Medical University of Vienna, Vienna, Austria.
Margot ErnstDepartment of Molecular Neurosciences, Center for Brain Research, Medical University of Vienna, Vienna, Austria.
James M CookDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, P.O. Box 413, Milwaukee, Wisconsin 53201, USA.
Miroslav M SavićDepartment of Pharmacology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: miroslav@pharmacy.bg.ac.rs.
University of Belgrade · RSMedical University of Vienna · ATUniversity of Wisconsin–Milwaukee · US

Funding

Development of new drugs for asthma by targeting GABA(A) receptors in the lungR01HL118561 · NHLBI · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2014 to 2017
$2.0M
Design of New Therapeutic Agents to Treat SchizophreniaR01MH096463 · NIMH · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2013 to 2017
$1.9M
Synthesis of Alpha2/Alpha3 GABA Agonists to Treat Neuropathic PainR01NS076517 · NINDS · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2012 to 2015
$1.3M
NHLBI NIH HHS R01 HL118561NIMH NIH HHS R01 MH096463NINDS NIH HHS R01 NS076517
6 · The paper itself

Abstract

We have synthesized and characterized MP-III-022 ((R)-8-ethynyl-6-(2-fluorophenyl)-N,4-dimethyl-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxamide) in vitro and in vivo as a binding- and efficacy-selective positive allosteric modulator of GABA

Indexed as

AmphetamineAnimalsDiazepamDrug StabilityElectrophysiological PhenomenaGABA-A Receptor AgonistsHand StrengthHEK293 CellsHumansImidazolesKineticsLocomotionMaleMaze LearningRatsRats, WistarAmphetamineDiazepamGABA-A Receptor AgonistsImidazolesReceptors, GABA-ASH-053-2'F-R-CH3Amide compoundBasic behaviorBinding assayFree brain concentrationRat kineticsReceptor efficacy

Identifiers

PMID27639297
PMCPMC5107132
OpenAlexW2518842266

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.