Evidence map›Paper›PMID 28011222›Full record

ArticleBioorganic & medicinal chemistry letters2017

Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.

Jason R Healy, Padmavani Bezawada, Nicholas W Griggs, Andrea L Devereaux, Rae R Matsumoto, John R Traynor, Andrew Coop, Christopher W Cunningham

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 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
–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

4 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
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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

8 authors.

Jason R HealyDepartment of Basic Pharmaceutical Sciences, West Virginia University School of Pharmacy, 2036 Health Sciences North, Morgantown, WV 26506, USA; Department of Pharmacology and Experimental Therapeutics, Thomas Jefferson University, 1170 Main Bldg., 132 S. 10th St., Philadelphia, PA 19107, USA.
Padmavani BezawadaDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, MD 21201, USA.
Nicholas W GriggsDepartment of Pharmacology, University of Michigan Medical School, 1220A MSRB, Ann Arbor, MI 48109, USA.
Andrea L DevereauxDepartment of Pharmaceutical Sciences, Concordia University Wisconsin School of Pharmacy, 12800 N. Lake Shore Drive, Mequon, WI 53097, USA.
Rae R MatsumotoDepartment of Basic Pharmaceutical Sciences, West Virginia University School of Pharmacy, 2036 Health Sciences North, Morgantown, WV 26506, USA; Department of Biological and Pharmaceutical Sciences, Touro University California College of Pharmacy, 1310 Club Drive, Vallejo, CA 94592, USA.
John R TraynorDepartment of Pharmacology, University of Michigan Medical School, 1220A MSRB, Ann Arbor, MI 48109, USA.
Andrew CoopDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, MD 21201, USA.
Christopher W CunninghamDepartment of Pharmaceutical Sciences, Concordia University Wisconsin School of Pharmacy, 12800 N. Lake Shore Drive, Mequon, WI 53097, USA. Electronic address: chris.cunningham@cuw.edu.

Funding

CLINICAL PHARMACOLOGY TRAINING PROGRAMT32GM008562 · NIGMS · THOMAS JEFFERSON UNIVERSITY · PI WALTER K KRAFT, Scott A. Waldman · 1995 to 2026
$10.2M
Allosteric Modulation of the Mu-Opioid ReceptorR37DA039997 · NIDA · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI TRAYNOR, JOHN R. · 2015 to 2024
$6.4M
OPIOIDS WITH DELTA ANTAGONIST AND MU AGONIST ACTIVITYR01DA013583 · NIDA · UNIVERSITY OF MARYLAND BALTIMORE · PI COOP, ANDREW · 2001 to 2012
$2.5M
Opioid Analgesics With Reduced ConstipationF31DA021049 · NIDA · UNIVERSITY OF MARYLAND BALTIMORE · PI CUNNINGHAM, CHRISTOPHER W · 2006 to 2008
$60k
NIDA NIH HHS F31 DA021049NIDA NIH HHS R01 DA013583NIDA NIH HHS R37 DA039997NIGMS NIH HHS T32 GM008562
6 · The paper itself

Abstract

Opioid analgesic tolerance remains a considerable drawback to chronic pain management. The finding that concomitant administration of delta opioid receptor (DOR) antagonists attenuates the development of tolerance to mu opioid receptor (MOR) agonists has led to interest in producing bifunctional MOR agonist/DOR antagonist ligands. Herein, we present 7-benzylideneoxymorphone (6, UMB 246) displaying MOR partial agonist/DOR antagonist activity, representing a new lead for designing bifunctional MOR/DOR ligands.

Indexed as

LigandsAnalgesicsAnimalsBenzylidene CompoundsMiceOxymorphonePainReceptors, Opioid, deltaReceptors, Opioid, mu7-benzylideneoxymorphoneAnalgesicsBenzylidene CompoundsLigandsOxymorphoneReceptors, Opioid, deltaReceptors, Opioid, muAnalgesic toleranceBenzylideneoxymorphoneDelta opioid receptorMu opioid receptorOxymorphone

Identifiers

PMID28011222
PMCPMC5404377

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.