Evidence map›Paper›PMID 32854311›Full record

ArticleMolecules (Basel, Switzerland)2020

A Structure-Activity Relationship Comparison of Imidazodiazepines Binding at Kappa, Mu, and Delta Opioid Receptors and the GABA

Guanguan Li, Amanda N Nieman, Md Yeunus Mian, Nicolas M Zahn, Brandon N Mikulsky, Michael M Poe, Kashi R Methuku, Yongfeng Liu, James M Cook, Douglas C Stafford and 1 more

Open access · goldAbstract readComparative Study
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.6field-weighted citation impact, top 35% 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

7 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
  2. Synthesis and Receptor Binding Studies of α5 GABAMolecules (Basel, Switzerland) · 2023
    Article
  3. Article
  4. Development of Inhaled GABAACS pharmacology & translational science · 2022
    Article
  5. Review
  6. Review
  7. 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 at 5 institutions in 2 countries.

Guanguan LiShenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis, Department of Chemistry, College of Science, Southern University of Science and Technology, Shenzhen 518055, China.ORCID 0000-0002-2284-0348
Amanda N NiemanDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee, Milwaukee, WI 53201, USA.
Md Yeunus MianDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee, Milwaukee, WI 53201, USA.
Nicolas M ZahnDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee, Milwaukee, WI 53201, USA.
Brandon N MikulskyPantherics Incorporated, La Jolla, CA 92037, USA.
Michael M PoeDepartment of Chemistry, Western Michigan University, Kalamazoo, MI 49008, USA.
Kashi R MethukuDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee, Milwaukee, WI 53201, USA.
Yongfeng LiuNational Institute of Mental Health Psychoactive Drug Screening Program, Department of Pharmacology, University of North Carolina Chapel Hill, Chapel Hill, NC 27599, USA.
James M CookDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee, Milwaukee, WI 53201, USA.ORCID 0000-0001-5512-3022
Douglas C StaffordDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee, Milwaukee, WI 53201, USA.
Leggy A ArnoldDepartment of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee, Milwaukee, WI 53201, USA.ORCID 0000-0003-1411-1572
University of Wisconsin–Milwaukee · USPanthera Corporation · USSouthern University of Science and Technology · CNUniversity of North Carolina at Chapel Hill · USWestern Michigan University · US

Funding

Synthesis of Alpha2/Alpha3 GABA Agonists to Treat Neuropathic PainR01NS076517 · NINDS · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2012 to 2015
$1.3M
A novel asthma drug candidate targeting the GABAergic system in lung inflammationR41HL147658 · NHLBI · PANTHERICS INCORPORATED · PI ARNOLD, ALEXANDER · 2019 to 2019
$225k
Small molecule inhibitors of the vitamin D receptor-coactivator interactionR03DA031090 · NIDA · UNIVERSITY OF WISCONSIN MILWAUKEE · PI ARNOLD, ALEXANDER · 2010 to 2011
$73k
Lynde and Harry Bradley Foundation n/aNational Science Foundation CHE-1625735NHLBI NIH HHS R41 HL147658NHLBI NIH HHS R41HL147658, R01HL118561NIDA NIH HHS R03 DA031090NINDS NIH HHS R01NS076517Richard and Ethel Herzfeld Foundation n/aUniversity of Wisconsin-Milwaukee catalyst grant
6 · The paper itself

Abstract

Analgesic and anti-inflammatory properties mediated by the κ opioid receptor (KOR) have been reported for oxadiazole imidazodiazepines. Affinities determined by radioligand competition assays of more than seventy imidazodiazepines using cell homogenates from HEK293 cells that overexpress KOR, µ opioid receptor (MOR), and δ opioid receptor (DOR) are presented. Affinities to synaptic, benzodiazepine-sensitive receptors (BZR) were determined with rat brain extract. The highest affinity for KOR was recorded for GL-I-30 (Ki of 27 nM) and G-protein recruitment was observed with an EC

Indexed as

AzepinesGABA-A Receptor AgonistsReceptors, GABA-AReceptors, Opioid, deltaReceptors, Opioid, kappaReceptors, Opioid, muAnimalsHEK293 CellsHumansProtein BindingStructure-Activity RelationshipAzepinesGABA-A Receptor AgonistsReceptors, GABA-AReceptors, Opioid, deltaReceptors, Opioid, kappaReceptors, Opioid, muGABAA receptorimidazodiazepineopioid receptor

Identifiers

PMID32854311
PMCPMC7503500
OpenAlexW3080873967

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.