Evidence map›Paper›PMID 38748608›Full record

ArticleJournal of medicinal chemistry2024

Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation.

Hina Andleeb, Roger L Papke, Clare Stokes, Katrin Richter, Sara M Herz, Ka Chiang, Siva R Raju Kanumuri, Abhisheak Sharma, M Imad Damaj, Veronika Grau and 2 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Article
  5. 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.

Hina AndleebDepartment of Chemistry, University of Florida, P.O. Box 117200, Gainesville, Florida 32611-7200, United States.ORCID 0000-0003-1992-6201
Roger L PapkeDepartment of Pharmacology and Therapeutics, University of Florida, P.O. Box 100267, Gainesville, Florida 32610, United States.ORCID 0000-0002-4468-8658
Clare StokesDepartment of Pharmacology and Therapeutics, University of Florida, P.O. Box 100267, Gainesville, Florida 32610, United States.
Katrin RichterDepartment of General and Thoracic Surgery, Laboratory of Experimental Surgery, Justus-Liebig-University, German Center for Lung Research [DZL], Cardio-Pulmonary Institute [CPI], Giessen 35385, Germany.
Sara M HerzDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia 23298, United States.
Ka ChiangDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia 23298, United States.
Siva R Raju KanumuriDepartment of Pharmaceutics, University of Florida, Gainesville, Florida 32610, United States.
Abhisheak SharmaDepartment of Pharmaceutics, University of Florida, Gainesville, Florida 32610, United States.
M Imad DamajDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia 23298, United States.
Veronika GrauDepartment of General and Thoracic Surgery, Laboratory of Experimental Surgery, Justus-Liebig-University, German Center for Lung Research [DZL], Cardio-Pulmonary Institute [CPI], Giessen 35385, Germany.
Nicole A HorensteinDepartment of Chemistry, University of Florida, P.O. Box 117200, Gainesville, Florida 32611-7200, United States.ORCID 0000-0001-7505-1230
Ganesh A ThakurDepartment of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, Bouvé College of Health Sciences, Northeastern University, Boston, Massachusetts 02115, United States.ORCID 0000-0002-7468-8819

Funding

Targeting of Alpha7 nAChR for therapeutic effectsR01GM057481 · NIGMS · UNIVERSITY OF FLORIDA · PI PAPKE, ROGER L · 2000 to 2023
$7.6M
NIGMS NIH HHS R01 GM057481
6 · The paper itself

Abstract

There is an urgent need for nonopioid treatments for chronic and neuropathic pain to provide effective alternatives amid the escalating opioid crisis. This study introduces novel compounds targeting the α9 nicotinic acetylcholine receptor (nAChR) subunit, which is crucial for pain regulation, inflammation, and inner ear functions. Specifically, it identifies novel substituted carbamoyl/amido/heteroaryl dialkylpiperazinium iodides as potent agonists selective for human α9 and α9α10 over α7 nAChRs, particularly compounds

Indexed as

AnalgesicsInflammationPiperazinesReceptors, NicotinicAnimalsHumansIodidesMaleMiceMice, KnockoutNicotinic AgonistsPainSaltsStructure-Activity RelationshipAnalgesicsCHRNA9 protein, humanIodidesNicotinic AgonistsPiperazinesReceptors, NicotinicSalts

Identifiers

PMID38748608
PMCPMC11181317

What Socratic 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 Socratic graph.