Evidence mapPaperPMID 36526469Full record

ArticleJournal of medicinal chemistry2023

Subnanomolar Affinity and Selective Antagonism at α7 Nicotinic Receptor by Combined Modifications of 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624).

Francesco Bavo, Marco Pallavicini, Susanna Pucci, Rebecca Appiani, Alessandro Giraudo, Hyoungil Oh, Dana L Kneisley, Brek Eaton, Linda Lucero, Cecilia Gotti and 3 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2023. 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
0.9field-weighted citation impact, top 28% 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, 11 citations in OpenAlex.

  1. Article
  2. Review
  3. Fluorescent Isostere (Journal of medicinal chemistry · 2025
    Article
  4. Article
  5. Review
  6. Article
  7. Review
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

13 authors at 5 institutions in 3 countries.

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
Hyoungil OhDepartment of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia 23298, United States.
Dana L KneisleyDepartment of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia 23298, United States.ORCID 0000-0003-4203-6872
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.
Francesco ClementiInstitute 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 Milan · ITNeuroscience Institute · ITVirginia Commonwealth University Medical Center · USBarrow Neurological Institute · USUniversity of Copenhagen · DK

Funding

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

Abstract

Modifications of the cationic head and the ethylene linker of 2-(triethylammonium)ethyl ether of 4-stilbenol (MG624) have been proved to produce selective α9*-nAChR antagonism devoid of any effect on the α7-subtype. Here, single structural changes at the styryl portion of MG624 lead to prevailing α7-nAChR antagonism without abolishing α9*-nAChR antagonism. Nevertheless, rigidification of the styryl into an aromatic bicycle, better if including a H-bond donor NH, such as 5-indolyl (

Indexed as

Receptors, Nicotinicalpha7 Nicotinic Acetylcholine ReceptorEtherEthersEthyl EthersQuaternary Ammonium CompoundsStilbenes4-hydroxystilbenealpha7 Nicotinic Acetylcholine ReceptorEtherEthersEthyl EthersQuaternary Ammonium CompoundsReceptors, NicotinicStilbenestriethyl-(beta-4-stilbenoxyethyl)ammonium

Identifiers

PMID36526469
PMCPMC9841521
OpenAlexW4311822747

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.