Evidence map›Paper›PMID 24761755›Full record

ArticleJournal of medicinal chemistry2014

Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.

Vinod Kumar, Irna E Ridzwan, Konstantinos Grivas, John W Lewis, Mary J Clark, Claire Meurice, Corina Jimenez-Gomez, Irina Pogozheva, Henry Mosberg, John R Traynor and 1 more

Open access · bronzeAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
0.7field-weighted citation impact, top 38% 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

10 citing papers in PubMed, 22 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Article
  6. Review
  7. Review
  8. Article
  9. Central N/OFQ-NOP Receptor System in Pain Modulation.Advances in pharmacology (San Diego, Calif.) · 2016
    Review
  10. 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

11 authors at 2 institutions in 2 countries.

Vinod KumarDepartment of Pharmacy and Pharmacology, University of Bath , Bath, BA2 7AY, U.K.
Irna E Ridzwan
Konstantinos Grivas
John W Lewis
Mary J Clark
Claire Meurice
Corina Jimenez-Gomez
Irina Pogozheva
Henry Mosberg
John R Traynor
Stephen M Husbands
University of Michigan–Ann Arbor · USUniversity of Bristol · GB

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
DISCOVERY OF NEW TREATMENTS FOR INTRAVENOUS DRUG ABUSER01DA007315 · NIDA · UNIVERSITY OF BRISTOL · PI HUSBANDS, STEPHEN M, TRAYNOR, JOHN R. · 1991 to 2019
$4.8M
TRAINING IN NEUROSCIENCE RELATED TO DRUG ABUSET32DA007315 · NIDA · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI HOOK, VIVIAN Y. H · 2000 to 2013
$2.7M
NIDA NIH HHS DA03910NIDA NIH HHS DA07315NIDA NIH HHS R01 DA003910NIDA NIH HHS R01 DA007315NIDA NIH HHS T32 DA007315
6 · The paper itself

Abstract

Emerging clinical and preclinical evidence suggests that a compound displaying high affinity for μ, κ, and δ opioid (MOP, KOP, and DOP) receptors and antagonist activity at each, coupled with moderate affinity and efficacy at nociceptin opioid peptide (NOP) receptors will have utility as a relapse prevention agent for multiple types of drug abuse. Members of the orvinol family of opioid ligands have the desired affinity profile but have typically displayed substantial efficacy at MOP and or KOP receptors. In this study it is shown that a phenyl ring analogue (1d) of buprenorphine displays the desired profile in vitro with high, nonselective affinity for the MOP, KOP, and DOP receptors coupled with moderate affinity for NOP receptors. In vivo, 1d lacked any opioid agonist activity and was an antagonist of both the MOP receptor agonist morphine and the KOP receptor agonist ethylketocyclazocine, confirming the desired opioid receptor profile in vivo.

Indexed as

Narcotic AntagonistsAnimalsBuprenorphineDrug DiscoveryLigandsMiceNociceptin ReceptorReceptors, OpioidStructure-Activity RelationshipBuprenorphineLigandsNarcotic AntagonistsNociceptin ReceptorOprl1 protein, mouseReceptors, Opioid

Identifiers

PMID24761755
PMCPMC4033651
OpenAlexW1977183398

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.