Evidence map›Paper›PMID 27933953›Full record

ArticleJournal of medicinal chemistry2016

Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABA

Michael M Poe, Kashi Reddy Methuku, Guanguan Li, Ashwini R Verma, Kelly A Teske, Douglas C Stafford, Leggy A Arnold, Jeffrey W Cramer, Timothy M Jones, Rok Cerne and 7 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
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 22 papers.

0numbers the graph read from it
0cells of the map it votes in
22citing papers in PubMed
2.7field-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

22 citing papers in PubMed, 47 citations in OpenAlex.

  1. Article
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  4. Antinociceptive Effects ofThe Journal of pharmacology and experimental therapeutics · 2024
    Article
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  7. Article
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  9. Article
  10. Review
  11. Article
  12. GABAJournal, genetic engineering & biotechnology · 2021
    Review
  13. Article
  14. 8-Substituted Triazolobenzodiazepines:Frontiers in pharmacology · 2021
    Article
  15. Article
  16. The Positive Allosteric Modulator ofThe Journal of pharmacology and experimental therapeutics · 2020
    Article
  17. Article
  18. The α2,3-selective potentiator of GABAPharmacology, biochemistry, and behavior · 2019
    Article
  19. Article
  20. 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

17 authors at 4 institutions in 3 countries.

Michael M PoeDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee , Milwaukee, Wisconsin 53201, United States.
Kashi Reddy MethukuDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee , Milwaukee, Wisconsin 53201, United States.
Guanguan LiDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee , Milwaukee, Wisconsin 53201, United States.
Ashwini R VermaDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee , Milwaukee, Wisconsin 53201, United States.
Kelly A TeskeDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee , Milwaukee, Wisconsin 53201, United States.
Douglas C StaffordDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee , Milwaukee, Wisconsin 53201, United States.
Leggy A ArnoldDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee , Milwaukee, Wisconsin 53201, United States.
Jeffrey W CramerLilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 42685, United States.
Timothy M JonesLilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 42685, United States.
Rok CerneLilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 42685, United States.
Michael J KrambisLilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 42685, United States.
Jeffrey M WitkinLilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 42685, United States.
Enrique JambrinaLilly Research Laboratories, Eli Lilly and Company , 28108 Alcobendas, Spain.
Sabah RehmanDepartment for Molecular Neurosciences, Medical University of Vienna , 1090 Vienna, Austria.
Margot ErnstDepartment for Molecular Neurosciences, Medical University of Vienna , 1090 Vienna, Austria.
James M CookDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee , Milwaukee, Wisconsin 53201, United States.
Jeffrey M SchkeryantzLilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 42685, United States.
University of Wisconsin–Milwaukee · USEli Lilly (United States) · USMedical University of Vienna · ATEli Lilly (Spain) · ES

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

1,4-Benzodiazepines are used in the treatment of anxiety disorders but have limited long-term use due to adverse effects. HZ-166 (2) has been shown to have anxiolytic-like effects with reduced sedative/ataxic liabilities. A 1,3-oxazole KRM-II-81 (9) was discovered from a series of six bioisosteres with significantly improved pharmacokinetic and pharmacodynamic properties as compared to 2. Oxazole 9 was further characterized and exhibited improved anxiolytic-like effects in a mouse marble burying assay and a rat Vogel conflict test.

Indexed as

AnimalsAnti-Anxiety AgentsAnxietyBenzodiazepinesDose-Response Relationship, DrugEpilepsyGABA-A Receptor AntagonistsHEK293 CellsHumansImidazolesLigandsMaleMiceMice, Inbred StrainsMolecular StructureOxazoles8-ethynyl-6-(2'-pyridine)-4H-2,5,10b-triazabenzo(e)azulene-3-carboxylic acid ethyl esterAnti-Anxiety AgentsBenzodiazepinesGABA-A Receptor AntagonistsImidazolesKRM-II-81LigandsOxazolesReceptors, GABA-A

Identifiers

PMID27933953
PMCPMC5215686
OpenAlexW2553945781

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.