ArticleBritish journal of pharmacology2012
Nociceptive and pro-inflammatory effects of dimethylallyl pyrophosphate via TRPV4 activation.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 57 citations in OpenAlex.
- A synthetic peptide, derived from neurotoxin GsMTx4, acts as a non-opioid analgesic to alleviate mechanical and neuropathic pain through the TRPV4 channel.Acta pharmaceutica Sinica. B · 2025Article
- Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.Current topics in medicinal chemistry · 2025Review
- Targeting TRPV4 Channels for Cancer Pain Relief.Cancers · 2024Review
- Gpr83 Tunes Nociceptor Function, Controlling Pain.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2023Article
- TRP Family Genes Are Differently Expressed and Correlated with Immune Response in Glioma.Brain sciences · 2022Article
- Physiological and Pathological Significance of Esophageal TRP Channels: Special Focus on TRPV4 in Esophageal Epithelial Cells.International journal of molecular sciences · 2022Review
- Emerging roles of keratinocytes in nociceptive transduction and regulation.Frontiers in molecular neuroscience · 2022Review
- Bisphosphonates Targeting Ion Channels and Musculoskeletal Effects.Frontiers in pharmacology · 2022Review
- Article
- TRPing on Cell Swelling - TRPV4 Senses It.Frontiers in immunology · 2021Review
- Transient receptor potential vanilloid 4 channels as therapeutic targets in diabetes and diabetes-related complications.Journal of diabetes investigation · 2020Review
- Role of Transient Receptor Potential Vanilloid 4 Channel in Skin Physiology and Pathology.Sultan Qaboos University medical journal · 2020Review
- Role of macrophage TRPV4 in inflammation.Laboratory investigation; a journal of technical methods and pathology · 2020Review
- Molecular mechanisms underlying the actions of arachidonic acid-derived prostaglandins on peripheral nociception.Journal of neuroinflammation · 2020Review
- Transient Receptor Potential Channels and Metabolism.Molecules and cells · 2019Review
- Transient receptor potential ion-channel subfamily V member 4: a potential target for cancer treatment.Cell death & disease · 2019Review
- TRPV4-Mediated Anti-nociceptive Effect of Suberanilohydroxamic Acid on Mechanical Pain.Molecular neurobiology · 2019Article
- Gut microbiota: Beyond metagenomics, metatranscriptomics illuminates microbiome functionality in IBD.Nature reviews. Gastroenterology & hepatology · 2018Article
- Dynamics of metatranscription in the inflammatory bowel disease gut microbiome.Nature microbiology · 2018Article
- Endogenous TRPV4 Expression of a Hybrid Neuronal Cell Line N18D3 and Its Utilization to Find a Novel Synthetic Ligand.Journal of molecular neuroscience : MN · 2017Article
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeSensory neuronal and epidermal transient receptor potential ion channels (TRPs) serve an important role as pain sensor molecules. While many natural and synthetic ligands for sensory TRPs have been identified, little is known about the endogenous activator for TRPV4. Recently, we reported that endogenous metabolites produced by the mevalonate pathway regulate the activities of sensory neuronal TRPs. Here, we show that dimethylallyl pyrophosphate (DMAPP), a substance produced by the same pathway is an activator of TRPV4. EXPERIMENTAL APPROACH: We examined the effects of DMAPP on sensory TRPs using Ca²⁺ imaging and whole-cell electrophysiology experiments with a heterologous expression system (HEK293T cells transfected with individual TRP channels), cultured sensory neurons and keratinocytes. We then evaluated nociceptive behavioural and inflammatory changes upon DMAPP administration in mice in vivo. KEY
resultsIn the HEK cell heterologous expression system, cultured sensory neurons and keratinocytes, µM concentrations of DMAPP activated TRPV4. Agonistic and antagonistic potencies of DMAPP for other sensory TRP channels were examined and activation of TRPV3 by camphor was found to be inhibited by DMAPP. In vivo assays, intraplantar injection of DMAPP acutely elicited nociceptive flinches that were prevented by pretreatment with TRPV4 blockers, indicating that DMAPP is a novel pain-producing molecule through TRPV4 activation. Further, DMAPP induced acute inflammation and noxious mechanical hypersensitivities in a TRPV4-dependent manner. CONCLUSIONS AND IMPLICATIONS: Overall, we found a novel sensory TRP acting metabolite and suggest that its use may help to elucidate the physiological role of TRPV4 in nociception and associated inflammation.
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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.