Evidence map›Paper›PMID 28796483›Full record

ArticleACS chemical neuroscience2017

Placement of Hydroxy Moiety on Pendant of Peptidomimetic Scaffold Modulates Mu and Kappa Opioid Receptor Efficacy.

Aubrie A Harland, Irina D Pogozheva, Nicholas W Griggs, Tyler J Trask, John R Traynor, Henry I Mosberg

Abstract readComparative Study
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS chemical neuroscience, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.7field-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

4 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. 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

6 authors at 1 institution in 1 country.

Aubrie A HarlandDepartment of Medicinal Chemistry, College of Pharmacy, University of Michigan , Ann Arbor, Michigan 48109, United States.
Irina D PogozhevaDepartment of Medicinal Chemistry, College of Pharmacy, University of Michigan , Ann Arbor, Michigan 48109, United States.
Nicholas W GriggsDepartment of Pharmacology, Medical School, University of Michigan , Ann Arbor, Michigan 48109, United States.
Tyler J TraskDepartment of Pharmacology, Medical School, University of Michigan , Ann Arbor, Michigan 48109, United States.
John R TraynorDepartment of Pharmacology, Medical School, University of Michigan , Ann Arbor, Michigan 48109, United States.
Henry I MosbergDepartment of Medicinal Chemistry, College of Pharmacy, University of Michigan , 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 NIH HHS R01 DA003910
6 · The paper itself

Abstract

In an effort to expand the structure-activity relationship (SAR) studies of a series of mixed-efficacy opioid ligands, peptidomimetics that incorporate methoxy and hydroxy groups around a benzyl or 2-methylindanyl pendant on a tetrahydroquinoline (THQ) core of the peptidomimetics were evaluated. Compounds containing a methoxy or hydroxy moiety in the o- or m-positions increased binding affinity to the kappa opioid receptor (KOR), whereas compounds containing methoxy or hydroxy groups in the p-position decreased KOR affinity and reduced or eliminated efficacy at the mu opioid receptor (MOR). The results from a substituted 2-methylindanyl series aligned with the findings from the substituted benzyl series. Our studies culminated in the development of 8c, a mixed-efficacy MOR agonist/KOR agonist with subnanomolar binding affinity for both MOR and KOR.

Indexed as

Analgesics, OpioidAnimalsCell Line, TumorCHO CellsCricetinaeCricetulusDrug Evaluation, PreclinicalEnkephalin, Ala(2)-MePhe(4)-Gly(5)-Enkephalin, D-Penicillamine (2,5)-Guanosine 5'-O-(3-Thiotriphosphate)HumansMiceNaloxonePeptidomimeticsProtein BindingProtein ConformationAnalgesics, OpioidEnkephalin, Ala(2)-MePhe(4)-Gly(5)-Enkephalin, D-Penicillamine (2,5)-Guanosine 5'-O-(3-Thiotriphosphate)NaloxonePeptidomimeticsReceptors, Opioid, deltaReceptors, Opioid, kappaReceptors, Opioid, mukappa opioid receptor agonistMixed-efficacy opioid ligandsmu opioid receptor agonistpeptidomimeticsstructure−activity relationships

Identifiers

PMID28796483
PMCPMC5691919
OpenAlexW2743642621

What OpenQuestion holds

Textmetadata
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.