Evidence map›Paper›PMID 38637015›Full record

ArticleThe Journal of pharmacology and experimental therapeutics2024

Low-Efficacy Mu Opioid Agonists as Candidate Analgesics: Effects of Novel C-9 Substituted Phenylmorphans on Pain-Depressed Behavior in Mice.

Edna J Santos, Hamid I Akbarali, Eric W Bow, Dana R Chambers, Eugene S Gutman, Arthur E Jacobson, Minho Kang, Young K Lee, Joshua A Lutz, Kenner C Rice and 2 more

Open access · bronzeAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in The Journal of pharmacology and experimental therapeutics, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.6field-weighted citation impact, top 18% 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

7 citing papers in PubMed, 6 citations in OpenAlex.

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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 1 country.

Edna J SantosDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).ORCID 0000-0002-3188-1061
Hamid I AkbaraliDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).ORCID 0000-0003-1423-0774
Eric W BowDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).
Dana R ChambersDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).
Eugene S GutmanDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).
Arthur E JacobsonDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).
Minho KangDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).
Young K LeeDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).
Joshua A LutzDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).
Kenner C RiceDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).ORCID 0000-0002-1147-9147
Agnieszka SulimaDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.).
S Stevens NegusDepartment of Pharmacology & Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, Virginia (E.J.S., H.I.A., M.K., Y.K.L., S.S.N.) and Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA and NIAAA, Bethesda, Maryland (E.W.B., D.R.C., E.S.G., A.E.J., J.A.L., K.C.R., A.S.) sidney.negus@vcuhealth.org.
Virginia Commonwealth University · USTarget (United States) · US

Funding

Medicinal Chemistry of Drugs Acting on Central and Peripheral Opioid ReceptorsZIADA000527 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI RICE, KENNER · 2009 to 2025
$23.2M
VCU Center for Drug Addiction ResearchP30DA033934 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI JILL C BETTINGER · 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
A Novel Assay to Improve Translation in Analgesic Drug DevelopmentR61NS133217 · NINDS · VIRGINIA COMMONWEALTH UNIVERSITY · PI NEGUS, SIDNEY S · 2023 to 2023
$244k
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 DA033934NIGMS NIH HHS R25 GM090084NINDS NIH HHS F31 NS122525NINDS NIH HHS R61 NS133217
6 · The paper itself

Abstract

Low-efficacy mu opioid receptor (MOR) agonists may serve as novel candidate analgesics with improved safety relative to high-efficacy opioids. This study used a recently validated assay of pain-depressed behavior in mice to evaluate a novel series of MOR-selective C9-substituted phenylmorphan opioids with graded MOR efficacies. Intraperitoneal injection of dilute lactic acid (IP acid) served as a noxious stimulus to depress locomotor activity by mice in an activity chamber composed of two compartments connected by an obstructed door. Behavioral measures included (1) crosses between compartments (vertical activity over the obstruction) and (2) movement counts quantified as photobeam breaks summed across compartments (horizontal activity). Each drug was tested alone and as a pretreatment to IP acid. A charcoal-meal test and whole-body-plethysmography assessment of breathing in 5% CO

Indexed as

Analgesics, OpioidBehavior, AnimalPainReceptors, Opioid, muAnalgesicsAnimalsDose-Response Relationship, DrugMaleMiceMotor ActivityAnalgesicsAnalgesics, OpioidReceptors, Opioid, mu

Identifiers

PMID38637015
PMCPMC11493441
OpenAlexW4394908669

What Socratic 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 Socratic graph.