Evidence map›Paper›PMID 34771099›Full record

ArticleMolecules (Basel, Switzerland)2021

Discovery of Novel Delta Opioid Receptor (DOR) Inverse Agonist and Irreversible (Non-Competitive) Antagonists.

Parthasaradhireddy Tanguturi, Vibha Pathak, Sixue Zhang, Omar Moukha-Chafiq, Corinne E Augelli-Szafran, John M Streicher

Erratum issuedOpen access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2021. 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 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
1.2field-weighted citation impact, top 23% 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

8 citing papers in PubMed, 14 citations in OpenAlex.

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4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

6 authors at 2 institutions in 1 country.

Parthasaradhireddy TanguturiDepartment of Pharmacology, College of Medicine, University of Arizona, Tucson, AZ 85724, USA.ORCID 0000-0002-2566-9312
Vibha PathakDepartment of Chemistry, Division of Drug Discovery, Southern Research Institute, Birmingham, AL 35205, USA.
Sixue ZhangDepartment of Chemistry, Division of Drug Discovery, Southern Research Institute, Birmingham, AL 35205, USA.
Omar Moukha-ChafiqDepartment of Chemistry, Division of Drug Discovery, Southern Research Institute, Birmingham, AL 35205, USA.
Corinne E Augelli-SzafranDepartment of Chemistry, Division of Drug Discovery, Southern Research Institute, Birmingham, AL 35205, USA.
John M StreicherDepartment of Pharmacology, College of Medicine, University of Arizona, Tucson, AZ 85724, USA.ORCID 0000-0002-4173-7362
Southern Research Institute · USUniversity of Arizona · US

Funding

Opioid Ligands for the treatment of Alzheimer's Disease (Administrative Supplement on Parent Grant R01DA038635)R01DA038635 · NIDA · SOUTHERN RESEARCH INSTITUTE · PI AUGELLI-SZAFRAN, CORINNE ELIZABETH · 2015 to 2019
$5.0M
NIH HHS R01DA038635NIH HHS R01DA038635-S1
6 · The paper itself

Abstract

The delta opioid receptor (DOR) is a crucial receptor system that regulates pain, mood, anxiety, and similar mental states. DOR agonists, such as SNC80, and DOR-neutral antagonists, such as naltrindole, were developed to investigate the DOR in vivo and as potential therapeutics for pain and depression. However, few inverse agonists and non-competitive/irreversible antagonists have been developed, and none are widely available. This leaves a gap in our pharmacological toolbox and limits our ability to investigate the biology of this receptor. Thus, we designed and synthesized the novel compounds SRI-9342 as an irreversible antagonist and SRI-45128 as an inverse agonist. These compounds were then evaluated in vitro for their binding affinity by radioligand binding, their functional activity by

Indexed as

Binding, CompetitiveDrug DiscoveryAnalgesics, OpioidChemistry Techniques, SyntheticHumansLigandsMolecular StructureProtein BindingReceptors, Opioid, deltaStructure-Activity RelationshipAnalgesics, OpioidLigandsReceptors, Opioid, deltadelta opioid receptorinverse agonistirreversible antagonistmolecular pharmacologynon-competitive antagonist

Identifiers

PMID34771099
PMCPMC8587863
OpenAlexW3214029509

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.