ArticlePLoS neglected tropical diseases2018
Activation of host transient receptor potential (TRP) channels by praziquantel stereoisomers.
Article in PLoS neglected tropical diseases, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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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.
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Who cites it
17 citing papers in PubMed, 23 citations in OpenAlex.
- Polypharmacology of anthelmintics at host and parasite ion channels.PLoS pathogens · 2026Article
- Progress interrogating TRPMPZQ as the target of praziquantel.PLoS neglected tropical diseases · 2024Review
- Metabolism of (R)-Praziquantel versus the Activation of a Parasite Transient Receptor Potential Melastatin Ion Channel.ChemMedChem · 2023Article
- Use the force, fluke: Ligand-independent gating of Schistosoma mansoni ion channel TRPMInternational journal for parasitology · 2023Article
- Natural variation in the binding pocket of a parasitic flatworm TRPM channel resolves the basis for praziquantel sensitivity.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Identification of Inhibitors of theACS medicinal chemistry letters · 2022Article
- Mechanism of praziquantel action at a parasitic flatworm ion channel.Science translational medicine · 2021Article
- Identification of novel modulators of a schistosome transient receptor potential channel targeted by praziquantel.PLoS neglected tropical diseases · 2021Article
- Activation of transient receptor potential channel Sm.(Schistosoma mansoni)TRPMParasitology research · 2020Review
- Schistosome TRP channels: An appraisal.International journal for parasitology. Drugs and drug resistance · 2020Review
- The Journey to Discovering a Flatworm Target of Praziquantel: A Long TRP.Trends in parasitology · 2020Review
- The anthelmintic drug praziquantel activates a schistosome transient receptor potential channel.The Journal of biological chemistry · 2019Article
- Anti-schistosomal action of the calcium channel agonist FPL-64176.International journal for parasitology. Drugs and drug resistance · 2019Article
- CaCold Spring Harbor perspectives in biology · 2019Review
- Recent Progress in TRPM8 Modulation: An Update.International journal of molecular sciences · 2019Review
- TRP channels as potential targets for antischistosomals.International journal for parasitology. Drugs and drug resistance · 2018Review
- Atypical pharmacology of schistosome TRPA1-like ion channels.PLoS neglected tropical diseases · 2018Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The anthelmintic praziquantel (±PZQ) serves as a highly effective antischistosomal therapy. ±PZQ causes a rapid paralysis of adult schistosome worms and deleterious effects on the worm tegument. In addition to these activities against the parasite, ±PZQ also modulates host vascular tone in blood vessels where the adult worms reside. In resting mesenteric arteries ±PZQ causes a constriction of basal tone, an effect mediated by (R)-PZQ activation of endogenous serotoninergic G protein coupled receptors (GPCRs). Here, we demonstrate a novel vasodilatory action of ±PZQ in mesenteric vessels that are precontracted by high potassium-evoked depolarization, an effect previously reported to be associated with agonists of the transient receptor potential melastatin 8 channel (TRPM8). Pharmacological profiling a panel of 17 human TRPs demonstrated ±PZQ activity against a subset of human TRP channels. Several host TRP channels (hTRPA1, hTRPC3, hTRPC7) were activated by both (R)-PZQ and (S)-PZQ over a micromolar range whereas hTRPM8 showed stereoselective activation by (S)-PZQ. The relaxant effect of ±PZQ in mesenteric arteries was caused by (S)-PZQ, and mimicked by TRPM8 agonists. However, persistence of both (S)-PZQ and TRPM8 agonist evoked vessel relaxation in TRPM8 knockout tissue suggested that canonical TRPM8 does not mediate this (S)-PZQ effect. We conclude that (S)-PZQ is vasoactive over the micromolar range in mesenteric arteries although the molecular mediators of this effect remain to be identified. These data expand our knowledge of the polypharmacology and host vascular efficacy of this clinically important anthelmintic.
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Registered trials
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.