Evidence map›Paper›PMID 31986033›Full record

ArticleJournal of medicinal chemistry2020

Aromatic-Amine Pendants Produce Highly Potent and Efficacious Mixed Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Peptidomimetics with Enhanced Metabolic Stability.

Sean Henry, Jessica P Anand, Jack J Twarozynski, Ashley C Brinkel, Irina D Pogozheva, Bryan F Sears, Emily M Jutkiewicz, John R Traynor, Henry I Mosberg

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
1.0field-weighted citation impact, top 29% 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

5 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
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  3. Review
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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 1 institution in 1 country.

Sean HenryDepartment of Medicinal Chemistry, College of Pharmacy , University of Michigan , 428 Church Street , Ann Arbor , Michigan 48109 , United States.
Jessica P AnandDepartment of Pharmacology, Medical School , University of Michigan , Ann Arbor , Michigan 48109 , United States.
Jack J TwarozynskiDepartment of Pharmacology, Medical School , University of Michigan , Ann Arbor , Michigan 48109 , United States.
Ashley C BrinkelDepartment of Pharmacology, Medical School , University of Michigan , Ann Arbor , Michigan 48109 , United States.
Irina D PogozhevaDepartment of Medicinal Chemistry, College of Pharmacy , University of Michigan , 428 Church Street , Ann Arbor , Michigan 48109 , United States.
Bryan F SearsDepartment of Pharmacology, Medical School , University of Michigan , Ann Arbor , Michigan 48109 , United States.
Emily M JutkiewiczDepartment of Pharmacology, Medical School , University of Michigan , Ann Arbor , Michigan 48109 , United States.
John R TraynorDepartment of Medicinal Chemistry, College of Pharmacy , University of Michigan , 428 Church Street , Ann Arbor , Michigan 48109 , United States.
Henry I MosbergDepartment of Medicinal Chemistry, College of Pharmacy , University of Michigan , 428 Church Street , Ann Arbor , Michigan 48109 , United States.ORCID 0000-0002-4107-8870
University of Michigan · US

Funding

Development of Mixed Function Opioid Peptides and PeptidomimeticsR01DA003910 · NIDA · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI MOSBERG, HENRY ISAAC · 1985 to 2017
$9.0M
NIDA Training Program in Neuroscience-Administrative SupplementT32DA007281 · NIDA · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Shelly Beth Flagel · 1995 to 2026
$5.7M
Examining Novel Fentalogs: Pharmacological Characteristics and ReversibilityR03DA048129 · NIDA · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ANAND, JESSICA PRIYA · 2019 to 2020
$156k
NIDA NIH HHS R01 DA003910NIDA NIH HHS R03 DA048129NIDA NIH HHS T32 DA007281
6 · The paper itself

Abstract

We previously reported a novel SAR campaign that converted a metabolically unstable series of μ-opioid receptor (MOR) agonist/δ-opioid receptor (DOR) antagonist bicyclic core peptidomimetics with promising analgesic activity and reduced abuse liabilities into a more stable series of benzylic core analogues. Herein, we expanded the SAR of that campaign and determined that the incorporation of amines into the benzylic pendant produces enhanced MOR-efficacy in this series, whereas the reincorporation of an aromatic ring into the pendant enhanced MOR-potency. Two compounds, which contain a piperidine (

Indexed as

Analgesics, OpioidAnimalsCHO CellsCricetulusMaleMice, Inbred C57BLMicrosomes, LiverMolecular StructurePeptidomimeticsReceptors, Opioid, deltaReceptors, Opioid, muStructure-Activity RelationshipAnalgesics, OpioidPeptidomimeticsReceptors, Opioid, deltaReceptors, Opioid, mu

Identifiers

PMID31986033
PMCPMC7047604
OpenAlexW3003457220

What OpenQuestion holds

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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.