Evidence map›Paper›PMID 25733887›Full record

ArticleProceedings of the National Academy of Sciences of the United States of America2015

Activation of TRPM3 by a potent synthetic ligand reveals a role in peptide release.

Katharina Held, Tatjana Kichko, Katrien De Clercq, Hugo Klaassen, Rieta Van Bree, Jean-Christophe Vanherck, Arnaud Marchand, Peter W Reeh, Patrick Chaltin, Thomas Voets and 1 more

Open access · bronzeAbstract read
In one paragraph

Article in Proceedings of the National Academy of Sciences of the United States of America, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 89 papers.

0numbers the graph read from it
0cells of the map it votes in
89citing papers in PubMed
5.8field-weighted citation impact, top 3% 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

89 citing papers in PubMed, 150 citations in OpenAlex.

  1. Article
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  6. Review
  7. Activation of TRPA1 and TRPM3 triggers CaThe Journal of physiology · 2025
    Article
  8. Article
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  14. Pregnenolone sulfate potentiates tetrodotoxin-resistant NaThe journal of headache and pain · 2025
    Article
  15. Review
  16. Article
  17. Article
  18. Article
  19. Article
  20. Navigating the Controversies: Role of TRPM Channels in Pain States.International journal of molecular sciences · 2024
    Review

29 more citing papers are in PubMed but not listed here.

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 4 institutions in 4 countries.

Katharina HeldLaboratory of Obstetrics and Experimental Gynecology and Laboratory of Ion Channel Research and Transient Receptor Potential Research Platform Leuven, Catholic University of Leuven, B-3000 Leuven, Belgium;
Tatjana KichkoInstitute of Physiology and Pathophysiology, University of Erlangen-Nuremberg, D-91054 Erlangen, Germany; and.
Katrien De ClercqLaboratory of Obstetrics and Experimental Gynecology and.
Hugo KlaassenCenter for Innovation and Stimulation of Drug Discovery Leuven and.
Rieta Van BreeLaboratory of Obstetrics and Experimental Gynecology and.
Jean-Christophe VanherckCenter for Innovation and Stimulation of Drug Discovery Leuven and.
Arnaud MarchandCenter for Innovation and Stimulation of Drug Discovery Leuven and.
Peter W ReehInstitute of Physiology and Pathophysiology, University of Erlangen-Nuremberg, D-91054 Erlangen, Germany; and.
Patrick ChaltinCenter for Innovation and Stimulation of Drug Discovery Leuven and Center for Drug Design and Discovery, Bio-Incubator 2, B-3001 Heverlee, Belgium.
Thomas VoetsLaboratory of Ion Channel Research and Transient Receptor Potential Research Platform Leuven, Catholic University of Leuven, B-3000 Leuven, Belgium;
Joris VriensLaboratory of Obstetrics and Experimental Gynecology and Joris.Vriens@med.kuleuven.be.
Institute of Experimental Endocrinology of the Slovak Academy of Sciences · SKKU Leuven · BEFriedrich-Alexander-Universität Erlangen-Nürnberg · DECenter for Innovation · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Transient receptor potential (TRP) cation channel subfamily M member 3 (TRPM3), a member of the TRP channel superfamily, was recently identified as a nociceptor channel in the somatosensory system, where it is involved in the detection of noxious heat; however, owing to the lack of potent and selective agonists, little is known about other potential physiological consequences of the opening of TRPM3. Here we identify and characterize a synthetic TRPM3 activator, CIM0216, whose potency and apparent affinity greatly exceeds that of the canonical TRPM3 agonist, pregnenolone sulfate (PS). In particular, a single application of CIM0216 causes opening of both the central calcium-conducting pore and the alternative cation permeation pathway in a membrane-delimited manner. CIM0216 evoked robust calcium influx in TRPM3-expressing somatosensory neurons, and intradermal injection of the compound induced a TRPM3-dependent nocifensive behavior. Moreover, CIM0216 elicited the release of the peptides calcitonin gene-related peptide (CGRP) from sensory nerve terminals and insulin from isolated pancreatic islets in a TRPM3-dependent manner. These experiments identify CIM0216 as a powerful tool for use in investigating the physiological roles of TRPM3, and indicate that TRPM3 activation in sensory nerve endings can contribute to neurogenic inflammation.

Indexed as

AnimalsCalciumCell Membrane PermeabilityHEK293 CellsHot TemperatureHumansInsulinInsulin-Secreting CellsInsulin SecretionIon Channel GatingLigandsMice, Inbred C57BLNerve EndingsNeuropeptidesNociceptionPainCalciumInsulinLigandsNeuropeptidesPregnenolonepregnenolone sulfateQuinolinesTRPM3 protein, mouseTRPM Cation Channelsnociceptorpeptide releaseTRP channelTRPM3

Identifiers

PMID25733887
PMCPMC4371942
OpenAlexW2044778710

What OpenQuestion holds

Textmetadata
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.