ArticleNaunyn-Schmiedeberg's archives of pharmacology2020
Desensitization of transient receptor potential vanilloid type-1 (TRPV1) channel as promising therapy of irritable bowel syndrome: characterization of the action of palvanil in the mouse gastrointestinal tract.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 21 citations in OpenAlex.
- Cannabigerol at the Interface of the Gut Microbiota and EndoCannabinoidome: Mechanistic Insights into Inflammation and Pain Modulation.Medical sciences (Basel, Switzerland) · 2026Review
- The Mast Cell-PAR2-TRP Axis: A Convergent Mechanism for Visceral Hypersensitivity Independent of Divergent Motility in IBS.Biomolecules · 2026Review
- Vitamin D3 mediates amelioration of ulcerative colitis via the TRPV1-MAPK signaling pathway.Frontiers in immunology · 2026Article
- Expression of transient receptor potential vanilloid type 1 (TRPV1) in colonic mucosa of patients with irritable bowel syndrome.American journal of translational research · 2025Article
- Chronic Gut Inflammation and Dysbiosis in IBS: Unraveling Their Contribution to Atopic Dermatitis Progression.International journal of molecular sciences · 2024Article
- TRPV1 participates in the protective effect of propolis on colonic tissue of ulcerative colitis.Zhong nan da xue xue bao. Yi xue ban = Journal of Central South University. Medical sciences · 2023Article
- Ingredients of Vicks VapoRub inhibit rhinovirus-induced ATP release.Drugs in context · 2023Article
- Role of Ion Channels in the Chemotransduction and Mechanotransduction in Digestive Function and Feeding Behavior.International journal of molecular sciences · 2022Review
- 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
- The Involvement of the Endogenous Opioid System in the Gastrointestinal Aging in Mice and Humans.International journal of molecular sciences · 2022Article
- The role of mechanosensitive ion channels in the gastrointestinal tract.Frontiers in physiology · 2022Review
- Computational Modeling to Explain Why 5,5-Diarylpentadienamides are TRPV1 Antagonists.Molecules (Basel, Switzerland) · 2021Article
- Sex-Bias in Irritable Bowel Syndrome: Linking Steroids to the Gut-Brain Axis.Frontiers in endocrinology · 2021Review
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Authors and funding
7 authors at 3 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
TRPV1 are involved in the control of the gastrointestinal (GI) functions and pain sensation. Their activation induces pain but it is followed by desensitization, which in turn causes analgesia. The studies from the last two decades indicate that TRPV1 are involved in visceral hypersensitivity in the GI tract and pathogenesis of irritable bowel syndrome (IBS). Therefore, the aim of this study is to assess the action of fast desensitizing agonist of TRPV1, palvanil (N-palmitoyl-vanillamine), in the murine GI tract and on nociception to evaluate its potential application in the therapy of IBS. The effect of palvanil on smooth muscle contractility was evaluated using organ baths. The impact of palvanil on intestinal secretion was assessed in Ussing chambers. In vivo, the action of palvanil (0.1-1 mg/kg) was assessed in whole GI transit, fecal pellet output, and colonic bead expulsion tests. The antinociceptive potency of palvanil was tested in the mustard oil-induced pain test. Palvanil inhibited colonic contractions (evoked by electrical field stimulation, EFS) and decreased the ion transport in the colon stimulated with forskolin. It did not affect secretion in experiments with veratridine. In vivo, palvanil prolonged whole GI transit at all doses tested. At the lower dose tested, it accelerated colonic motility during first 60 min following injection. By contrast, at the dose of 1 mg/kg, colonic motility was inhibited. Palvanil induced antinociceptive action at all tested doses in mustard oil-induced pain test. TRPV1 fast-desensitizing compounds, i.e., palvanil, may be promising agents in the therapy of IBS since it modulates intestinal motility and reduces visceral pain.
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