Evidence map›Paper›PMID 27631130›Full record

ArticlePharmaceutical research2016

Niclosamide is a Negative Allosteric Modulator of Group I Metabotropic Glutamate Receptors: Implications for Neuropathic Pain.

Ni Ai, Richard D Wood, Eric Yang, William J Welsh

Abstract read
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In one paragraph

Article in Pharmaceutical research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
1.0field-weighted citation impact, top 26% 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

13 citing papers in PubMed, 18 citations in OpenAlex.

  1. Trial
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  7. Acta pharmaceutica Sinica. B · 2024
    Review
  8. Integrated Computational Approaches and Tools forAllosteric Drug Discovery.International journal of molecular sciences · 2020
    Review
  9. Article
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  12. Review
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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

4 authors at 3 institutions in 2 countries.

Ni AiPharmaceutical Informatics Institute, College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Road, Hangzhou, Zhejiang, 310058, People's Republic of China.
Richard D WoodSnowdon, Inc., Princeton, New Jersey, 08540, USA.
Eric YangSnowdon, Inc., Princeton, New Jersey, 08540, USA.
William J WelshDepartment of Pharmacology, Rutgers-Robert Wood Johnson Medical School, Rutgers University, 661 Hoes Lane West, Staged Research Building (room SRB-124), Piscataway, New Jersey, 08854, USA. welshwj@rwjms.rutgers.edu.
Snowdon (United States) · USRutgers, The State University of New Jersey · USZhejiang University · CN

Funding

Translational Research Support CoreP30ES005022 · NIEHS · UNIV OF MED/DENT NJ-R W JOHNSON MED SCH · PI ROBERT John LAUMBACH · 1988 to 2026
$47.4M
NIEHS NIH HHS P30 ES005022
6 · The paper itself

Abstract

purposeNovel therapeutics are greatly needed that target specific pathological receptors and pathways involved in Neuropathic Pain (NP). Extending our previous work published in this Journal on Group I metabotropic glutamate receptor (mGluR) modulators, we now investigate the therapeutic potential of niclosamide in modulating aberrant glutamate transmission in NP.

methodCalcium mobilization assays and cross-receptor selectivity experiments are conducted to characterize the pharmacological activity of niclosamide. A focused series of niclosamide analogues is then prepared to elucidate key structural determinants that emerged from computational molecular modeling analysis on drug-receptor interactions. Finally, niclosamide and a carbamate derivative are studied to assess their efficacy in an NP-evoked mechanical hyperalgesia model in rats.

resultsNiclosamide is a low-nanomolar allosteric antagonist of Group I mGluRs with high selectivity for Group I over homologous Group III mGluRs. The phenolic hydroxyl group of niclosamide forms a crucial hydrogen bond with mGluR1/5. Its bioactive coplanar conformation is further stabilized by the nitro substituent on the B ring and an intramolecular bond. Mechanical hyperalgesia in NP rats is reversed by niclosamide through three different dosing routes.

conclusionTo our knowledge, this is the first report of the salicylanilide class of compounds as potential treatments for NP.

Indexed as

Allosteric RegulationAnalgesicsAnimalsCell LineHumansHyperalgesiaMaleMolecular Docking SimulationNeuralgiaNiclosamideRats, Sprague-DawleyReceptor, Metabotropic Glutamate 5Receptors, Metabotropic GlutamateAnalgesicsmetabotropic glutamate receptor type 1NiclosamideReceptor, Metabotropic Glutamate 5Receptors, Metabotropic Glutamategroup I metabotropic glutamate receptorsneuropathic painniclosamide

Identifiers

PMID27631130
OpenAlexW2508056133

What OpenQuestion holds

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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 OpenQuestion graph.