Evidence map›Paper›PMID 37381112›Full record

ArticlePharmacology research & perspectives2023

Role of efficacy as a determinant of locomotor activation by mu-opioid receptor (MOR) ligands in female and male mice. II. Effects of novel MOR-selective phenylmorphans with high-to-low MOR efficacy.

Edna J Santos, Nima Nassehi, Eric W Bow, Dana R Chambers, Eugene S Gutman, Arthur E Jacobson, Joshua A Lutz, Samuel A Marsh, Kenner C Rice, Agnieszka Sulima and 2 more

Open access · goldAbstract read
In one paragraph

Article in Pharmacology research & perspectives, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
1.6field-weighted citation impact, top 17% 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

12 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Review
  5. Classics in Chemical Neuroscience: Tianeptine.ACS chemical neuroscience · 2024
    Review
  6. Article
  7. Article
  8. Article
  9. Article
  10. 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

12 authors at 2 institutions in 2 countries.

Edna J SantosDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA.
Nima NassehiDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA.
Eric W BowDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA.
Dana R ChambersDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA.
Eugene S GutmanDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA.
Arthur E JacobsonDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA.
Joshua A LutzDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA.
Samuel A MarshDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA.
Kenner C RiceDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA.
Agnieszka SulimaDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland, USA.
Dana E SelleyDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA.
S Stevens NegusDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA.ORCID 0000-0001-8471-645X
Chemical Synthesis Lab · SGVirginia Commonwealth University · US

Funding

TRAINING IN THE PHARMACOLOGY OF ABUSED DRUGST32DA007027 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI William L. Dewey · 1985 to 2026
$14.7M
VCU Center for Drug Addiction ResearchP30DA033934 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI ARON H LICHTMAN · 2014 to 2026
$13.8M
Virginia Commonwealth University Initiative for Maximizing Student DevelopmentR25GM090084 · NIGMS · VIRGINIA COMMONWEALTH UNIVERSITY · PI AKBARALI, HAMID I, LLOYD, JOYCE A. · 2010 to 2022
$5.2M
Intrinsic Efficacy as a Determinant of Opioid Effectiveness in Treatment of Pain-Depressed BehaviorF31NS122525 · NINDS · VIRGINIA COMMONWEALTH UNIVERSITY · PI EVINGTON, EDNA J · 2022 to 2023
$59k
NIDA NIH HHS P30 DA033934NIDA NIH HHS T32 DA007027NIGMS NIH HHS R25 GM090084NINDS NIH HHS F31 NS122525
6 · The paper itself

Abstract

Low-efficacy mu-opioid receptor (MOR) agonists represent promising therapeutics, but existing compounds (e.g., buprenorphine, nalbuphine) span a limited range of low MOR efficacies and have poor MOR selectivity. Accordingly, new and selective low-efficacy MOR agonists are of interest. A novel set of chiral C9-substituted phenylmorphans has been reported to display improved MOR selectivity and a range of high-to-low MOR efficacies under other conditions; however, a full opioid receptor binding profile for these drugs has not been described. Additionally, studies in mice will be useful for preclinical characterization of these novel compounds, but the pharmacology of these drugs in mice has also not been examined. Accordingly, the present study characterized the binding selectivity and in vitro efficacy of these compounds using assays of opioid receptor binding and ligand-stimulated [

Indexed as

Analgesics, OpioidBuprenorphineReceptors, Opioid, muAnimalsFemaleGuanosine 5'-O-(3-Thiotriphosphate)LigandsMaleMiceMorphinansThiazepinesAnalgesics, OpioidBuprenorphineGuanosine 5'-O-(3-Thiotriphosphate)LigandsMorphinansphenylmorphanReceptors, Opioid, muThiazepinestianeptineefficacylocomotor activitymousemu opioid receptoropioidreceptor binding

Identifiers

PMID37381112
PMCPMC10307939
OpenAlexW4382501526

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.