Evidence map›Paper›PMID 31779072›Full record

ArticleMolecules (Basel, Switzerland)2019

Structure-Activity Relationships of 7-Substituted Dimethyltyrosine-Tetrahydroisoquinoline Opioid Peptidomimetics.

Deanna Montgomery, Jessica P Anand, Mason A Baber, Jack J Twarozynski, Joshua G Hartman, Lennon J Delong, John R Traynor, Henry I Mosberg

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
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

1 citing paper in PubMed.

  1. 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

8 authors.

Deanna MontgomeryDepartment of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109, USA.ORCID 0000-0002-6181-3131
Jessica P AnandDepartment of Pharmacology, Medical School, University of Michigan, Ann Arbor, MI 48109, USA.
Mason A BaberDepartment of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109, USA.
Jack J TwarozynskiDepartment of Pharmacology, Medical School, University of Michigan, Ann Arbor, MI 48109, USA.
Joshua G HartmanDepartment of Pharmacology, Medical School, University of Michigan, Ann Arbor, MI 48109, USA.
Lennon J DelongDepartment of Pharmacology, Medical School, University of Michigan, Ann Arbor, MI 48109, USA.
John R TraynorDepartment of Pharmacology, Medical School, University of Michigan, Ann Arbor, MI 48109, USA.
Henry I MosbergDepartment of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109, USA.

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
Development of Long Lasting Stable Fentanyl Antagonist to Reverse Opioid OverdoseR21DA051732 · NIDA · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ANAND, JESSICA PRIYA · 2020 to 2021
$429k
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 DA003910NIDA NIH HHS R03 DA048129NIDA NIH HHS R21 DA051732
6 · The paper itself

Abstract

The opioid receptors modulate a variety of biological functions, including pain, mood, and reward. As a result, opioid ligands are being explored as potential therapeutics for a variety of indications. Multifunctional opioid ligands, which act simultaneously at more than one type of opioid receptor, show promise for use in the treatment of addiction, pain, and other conditions. Previously, we reported the creation of bifunctional kappa opioid receptor (KOR) agonist/mu opioid receptor (MOR) partial agonist ligands from the classically delta opioid receptor (DOR) antagonist selective dimethyltyrosine-tetrahydroisoquinoline (Dmt-Tiq) scaffold through the addition of a 7-benzyl pendant on the tetrahydroisoquinoline ring. This study further explores the structure-activity relationships surrounding 7-position pendants on the Dmt-Tiq scaffold. Some analogues maintain a KOR agonist/MOR partial agonist profile, which is being explored in the development of a treatment for cocaine addiction. Others display a MOR agonist/DOR antagonist profile, which has potential to be used in the creation of a less addictive pain medication. Ultimately, we report the synthesis and in vitro evaluation of novel opioid ligands with a variety of multifunctional profiles.

Indexed as

Analgesics, OpioidAnimalsCell LineCHO CellsCricetulusHumansPainPain ManagementPeptidomimeticsReceptors, OpioidStructure-Activity RelationshipTetrahydroisoquinolinesAnalgesics, OpioidPeptidomimeticsReceptors, OpioidTetrahydroisoquinolinesmultifunctional ligandsopioidspeptidomimeticstructure-activity

Identifiers

PMID31779072
PMCPMC6930500

What OpenQuestion holds

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LicenceCC BY
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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.