Evidence mapPaperPMID 35834819Full record

ArticleJournal of medicinal chemistry2022

From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human α9α10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.

Francesco Bavo, Marco Pallavicini, Susanna Pucci, Rebecca Appiani, Alessandro Giraudo, Brek Eaton, Linda Lucero, Cecilia Gotti, Milena Moretti, Paul Whiteaker and 1 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing 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

8 citing papers in PubMed, 0 citations in OpenAlex.

  1. Article
  2. Article
  3. Fluorescent Isostere (Journal of medicinal chemistry · 2025
    Article
  4. Article
  5. Analogs of α-conotoxin PnIC selectively inhibit α7β2- over α7-only subtype nicotinic acetylcholine receptors via a novel allosteric mechanism.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2024
    Article
  6. Article
  7. Review
  8. 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 1 institution in 1 country.

Francesco BavoDipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, via Mangiagalli 25, I-20133 Milano, Italy.
Marco PallaviciniDipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, via Mangiagalli 25, I-20133 Milano, Italy.ORCID 0000-0003-3344-484X
Susanna PucciInstitute of Neuroscience, CNR, via Vanvitelli 32, I-20129 Milano, Italy.
Rebecca AppianiDipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, via Mangiagalli 25, I-20133 Milano, Italy.
Alessandro GiraudoDipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, via Mangiagalli 25, I-20133 Milano, Italy.ORCID 0000-0002-5291-0837
Brek EatonDivision of Neurobiology, Barrow Neurological Institute, Phoenix, Arizona 85013, United States.
Linda LuceroDivision of Neurobiology, Barrow Neurological Institute, Phoenix, Arizona 85013, United States.
Cecilia GottiInstitute of Neuroscience, CNR, via Vanvitelli 32, I-20129 Milano, Italy.
Milena MorettiInstitute of Neuroscience, CNR, via Vanvitelli 32, I-20129 Milano, Italy.
Paul WhiteakerDepartment of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia 23298, United States.
Cristiano BolchiDipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, via Mangiagalli 25, I-20133 Milano, Italy.ORCID 0000-0002-6726-9501
University of California, San Diego · US

Funding

NIDA NIH HHS R01 DA042749NIDA NIH HHS R01 DA043567
6 · The paper itself

Abstract

Nicotinic acetylcholine receptors containing α9 subunits (α9*-nAChRs) are potential druggable targets arousing great interest for pain treatment alternative to opioids. Nonpeptidic small molecules selectively acting as α9*-nAChRs antagonists still remain an unattained goal. Here, through modifications of the cationic head and the ethylene linker, we have converted the 2-triethylammonium ethyl ether of 4-stilbenol (MG624), a well-known α7- and α9*-nAChRs antagonist, into some selective antagonists of human α9*-nAChR. Among these, the compound with cyclohexyldimethylammonium head (

Indexed as

Ammonium CompoundsReceptors, NicotinicEtherHumansNicotinic AntagonistsQuaternary Ammonium CompoundsStilbenes4-hydroxystilbeneAmmonium CompoundsEtherNicotinic AntagonistsQuaternary Ammonium CompoundsReceptors, NicotinicStilbenestriethyl-(beta-4-stilbenoxyethyl)ammonium

Identifiers

PMID35834819
PMCPMC9339509
OpenAlexW35834819

What Socratic holds

Textmetadata
LicenceCC BY
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.