ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2010
Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermia.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 75 papers.
What it found
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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.
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Who cites it
75 citing papers in PubMed, 160 citations in OpenAlex.
- Effect of analgesic therapy on clinical outcome measures in a randomized controlled trial using client-owned dogs with hip osteoarthritis.BMC veterinary research · 2012Trial
- An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects.British journal of clinical pharmacology · 2011Trial
- Identification of a human mitochondrial isoform of TRPV1: a thermostat regulating mitochondrial maximal temperature?Cellular and molecular life sciences : CMLS · 2026Article
- Supercritical COPharmaceutics · 2026Article
- TRPV1 mediates mitochondrial dysfunction in hyperthermia-induced ameloblast mineralization defects.Frontiers in cell and developmental biology · 2026Article
- An adamantane-based ligand as a novel chemical tool for thermosensory TRPM8 channel therapeutic modulation.The FEBS journal · 2025Article
- iPSC-derived human sensory neurons reveal a subset of TRPV1 antagonists as anti-pruritic compounds.Scientific reports · 2024Article
- GLP-1 and its derived peptides mediate pain relief through direct TRPV1 inhibition without affecting thermoregulation.Experimental & molecular medicine · 2024Article
- GLP-1 and Its Derived Peptides Mediate Pain Relief Through Direct TRPV1 Inhibition Without Affecting Thermoregulation.Research square · 2024Article
- Transient receptor potential vanilloid 1: A potential therapeutic target for the treatment of osteoarthritis and rheumatoid arthritis.Cell proliferation · 2024Review
- Striving toward hyperthermia-free analgesia: lessons from loss-of-function mutations of human TRPV1.The Journal of clinical investigation · 2023Article
- Progress in the Structural Basis of thermoTRP Channel Polymodal Gating.International journal of molecular sciences · 2023Review
- The neural pathway of the hyperthermic response to antagonists of the transient receptor potential vanilloid-1 channel.Temperature (Austin, Tex.) · 2023Article
- Genetically-encoded BRET probes shed light on ligand bias-induced variable ion selectivity in TRPV1 and P2X5/7.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- TRPV1 drugs alter core body temperature via central projections of primary afferent sensory neurons.eLife · 2022Article
- Venom Peptide Toxins Targeting the Outer Pore Region of Transient Receptor Potential Vanilloid 1 in Pain: Implications for Analgesic Drug Development.International journal of molecular sciences · 2022Review
- Nociception and hypersensitivity involve distinct neurons and molecular transducers inProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Sensitization of primary cultures from rat dorsal root ganglia with lipopolysaccharide (LPS) requires a robust inflammatory response.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2022Article
- Rational Design of a Modality-Specific Inhibitor of TRPM8 Channel against Oxaliplatin-Induced Cold Allodynia.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2021Article
- Mice lacking endogenous TRPV1 express reduced levels of thermogenic proteins and are susceptible to diet-induced obesity and metabolic dysfunction.FEBS letters · 2021Article
15 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
Abstract
Transient receptor potential vanilloid-1 (TRPV1) antagonists are widely viewed as next-generation pain therapeutics. However, these compounds cause hyperthermia, a serious side effect. TRPV1 antagonists differentially block three modes of TRPV1 activation: by heat, protons, and chemical ligands (e.g., capsaicin). We asked what combination of potencies in these three modes of TRPV1 activation corresponds to the lowest potency of a TRPV1 antagonist to cause hyperthermia. We studied hyperthermic responses of rats, mice, and guinea pigs to eight TRPV1 antagonists with different pharmacological profiles and used mathematical modeling to find a relative contribution of the blockade of each activation mode to the development of hyperthermia. We found that the hyperthermic effect has the highest sensitivity to the extent of TRPV1 blockade in the proton mode (0.43 to 0.65) with no to moderate sensitivity in the capsaicin mode (-0.01 to 0.34) and no sensitivity in the heat mode (0.00 to 0.01). We conclude that hyperthermia-free TRPV1 antagonists do not block TRPV1 activation by protons, even if they are potent blockers of the heat mode, and that decreasing the potency to block the capsaicin mode may further decrease the potency to cause hyperthermia.
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What OpenQuestion holds
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.