Evidence map›Paper›PMID 39698260›Full record

ArticleACS pharmacology & translational science2024

Discovery of 6α-Thiazolylcarboxamidonaltrexamine Derivative (NTZ) as a Potent and Central Nervous System Penetrant Opioid Receptor Modulator with Drug-like Properties for Potential Treatment of Opioid Use Disorder.

Boshi Huang, Hongguang Ma, Piyusha P Pagare, Mengchu Li, Rolando E Mendez, James C Gillespie, Justin L Poklis, Matthew S Halquist, David L Stevens, William L Dewey and 2 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS pharmacology & translational science, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

12 authors.

Boshi HuangDepartment of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia23298, United States.
Hongguang MaDepartment of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia23298, United States.
Piyusha P PagareDepartment of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia23298, United States.ORCID https://orcid.org/0000-0002-4848-2673
Mengchu LiDepartment of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia23298, United States.ORCID https://orcid.org/0000-0002-2551-2155
Rolando E MendezDepartment of Pharmacology and Toxicology, School of Medicine, Virginia Commonwealth University, 410 North 12th Street, Richmond, Virginia23298, United States.
James C GillespieDepartment of Pharmacology and Toxicology, School of Medicine, Virginia Commonwealth University, 410 North 12th Street, Richmond, Virginia23298, United States.
Justin L PoklisDepartment of Pharmacology and Toxicology, School of Medicine, Virginia Commonwealth University, 410 North 12th Street, Richmond, Virginia23298, United States.
Matthew S HalquistDepartment of Pharmaceutics, Virginia Commonwealth University, 410 North 12th Street, Richmond, Virginia23298, United States.
David L StevensDepartment of Pharmacology and Toxicology, School of Medicine, Virginia Commonwealth University, 410 North 12th Street, Richmond, Virginia23298, United States.
William L DeweyDepartment of Pharmacology and Toxicology, School of Medicine, Virginia Commonwealth University, 410 North 12th Street, Richmond, Virginia23298, United States.
Dana E SelleyDepartment of Pharmacology and Toxicology, School of Medicine, Virginia Commonwealth University, 410 North 12th Street, Richmond, Virginia23298, United States.
Yan ZhangDepartment of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia23298, United States.ORCID https://orcid.org/0000-0001-8934-7016

Funding

VCU Center for Drug Addiction ResearchP30DA033934 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI JOLENE J WINDLE · 2014 to 2026
$13.8M
Mu Opioid Receptor Modulator Development to Treat Opioid Use DisorderUH3DA050311 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI ZHANG, YAN · 2023 to 2025
$4.3M
Non-peptide Mu Opioid Receptor Selective AntagonistsR01DA024022 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI ZHANG, YAN · 2009 to 2019
$3.5M
Bivalent Ligands as Chemical Probes to Study Opioid Abuse-enhanced HIV InfectionR01DA044855 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI HAUSER, KURT F, ZHANG, YAN · 2017 to 2021
$2.7M
Novel fentanyl derivatives as counteracting agents against fentanylUG3DA050311 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI ZHANG, YAN · 2019 to 2020
$2.2M
NIDA NIH HHS P30 DA033934NIDA NIH HHS R01 DA024022NIDA NIH HHS R01 DA044855NIDA NIH HHS UG3 DA050311NIDA NIH HHS UH3 DA050311
6 · The paper itself

Abstract

The development of highly potent and selective μ opioid receptor (MOR) modulators with favorable drug-like properties has always been a focus in the opioid domain. Our previous efforts led to the discovery of a lead compound designated as NAT, a potent centrally acting MOR modulator. However, the fact that NAT precipitated considerable withdrawal effects at higher doses largely impaired its further development. In the light of the concept of activity cliff and CNS multiparameter optimization algorithm, a nitrogen atom was incorporated into the thiophene ring of NAT, aiming to preserve desirable pharmacological activities and CNS permeability while alleviating withdrawal symptoms. Among all 16 new analogs, compound

Identifiers

PMID39698260
PMCPMC11651181

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Registered trials

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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.