ArticleBritish journal of pharmacology2005
Effects of piperine, the pungent component of black pepper, at the human vanilloid receptor (TRPV1).
Article in British journal of pharmacology, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 96 papers, 2 of them syntheses that pooled it.
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Who cites it
96 citing papers in PubMed, 2 syntheses or guidelines pooled it, 305 citations in OpenAlex.
- Modulation of transient receptor potential (TRP) channels by plant derived substances used in over-the-counter cough and cold remedies.Respiratory research · 2023Pooled it
- The Impact of TRPV1 on Cancer Pathogenesis and Therapy: A Systematic Review.International journal of biological sciences · 2021Pooled it
- Article
- Piperine disrupts the OFF state of the resting thick filament of rat skeletal muscle, enhancing dynamic contractility in a fibre-type-dependent manner.The Journal of physiology · 2026Article
- A double-blinded randomized clinical trial: Topical Sahasthara extractJournal of traditional and complementary medicine · 2026Article
- Topical Piperine for the Management of Burning Mouth Syndrome: A Case Series.Journal of clinical medicine · 2026Article
- Piperine-primed rat mesenchymal stem cells' secretome promotes an anti-inflammatory phenotype in the J774.1 murine macrophage cell line.Genes & nutrition · 2026Article
- High-concentration (8%) capsaicin patch for chronic postoperative neuropathic pain: A systematic review of randomised controlled trials.British journal of pain · 2025Article
- Physiological functions and pharmacological targeting of transient receptor potential channels.Pharmacological reviews · 2025Review
- Microemulsion-based drug delivery system identifies pepper alkaloids as anti-obesity compounds.Acta pharmacologica Sinica · 2025Article
- A Comprehensive Review on Plant-Based Medications and Chemical Approaches for Autism Spectrum Disorders (ASDs) Psychopharmacotherapy.Indian journal of microbiology · 2025Article
- Novel Perspectives for Sensory Analysis Applied to Piperaceae and Aromatic Herbs: A Pilot Study.Foods (Basel, Switzerland) · 2025Article
- Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.Current topics in medicinal chemistry · 2025Review
- Pharmacology of Non-Psychoactive Phytocannabinoids and Their Potential for Treatment of Cardiometabolic Disease.Handbook of experimental pharmacology · 2025Review
- Sensory-Motor Neuropathy in Mfn2 T105M Knock-in Mice and Its Reversal by a Novel Piperine-Derived Mitofusin Activator.The Journal of pharmacology and experimental therapeutics · 2024Article
- Capsaicin: Emerging Pharmacological and Therapeutic Insights.Current issues in molecular biology · 2024Review
- Subunit-specific inhibition of BK channels by piperine.Biophysical journal · 2024Article
- Magnetogenetic cell activation using endogenous ferritin.bioRxiv : the preprint server for biology · 2024Article
- The effect of turmeric and black pepper powder incorporated in breakfast on postprandial glycemia, appetite, palatability, and gastrointestinal well-being in normal-weight adults.Food science & nutrition · 2024Article
- A Stable Cell Line Co-expressing hTRPV1 and GCaMP6s: A Novel Cell-based Assay For High-throughput Screening of hTRPV1 Agonists.Combinatorial chemistry & high throughput screening · 2024Article
36 more citing papers are in PubMed but not listed here.
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. We have characterised the effects of piperine, a pungent alkaloid found in black pepper, on the human vanilloid receptor TRPV1 using whole-cell patch-clamp electrophysiology. 2. Piperine produced a clear agonist activity at the human TRPV1 receptor yielding rapidly activating whole-cell currents that were antagonised by the competitive TRPV1 antagonist capsazepine and the non-competitive TRPV1 blocker ruthenium red. 3. The current-voltage relationship of piperine-activated currents showed pronounced outward rectification (25+/-4-fold between -70 and +70 mV) and a reversal potential of 0.0+/-0.4 mV, which was indistinguishable from that of the prototypical TRPV1 agonist capsaicin. 4. Although piperine was a less potent agonist (EC50=37.9+/-1.9 microM) than capsaicin (EC50=0.29+/-0.05 microM), it demonstrated a much greater efficacy (approximately two-fold) at TRPV1. 5. This difference in efficacy did not appear to be related to the proton-mediated regulation of the receptor since a similar degree of potentiation was observed for responses evoked by piperine (230+/-20%, n=11) or capsaicin (284+/-32%, n=8) upon acidification to pH 6.5. 6. The effects of piperine upon receptor desensitisation were also unable to explain this effect since piperine resulted in more pronounced macroscopic desensitisation (t(1/2)=9.9+/-0.7 s) than capsaicin (t(1/2)>20 s) and also caused greater tachyphylaxis in response to repetitive agonist applications. 7. Overall, our data suggest that the effects of piperine at human TRPV1 are similar to those of capsaicin except for its propensity to induce greater receptor desensitisation and, rather remarkably, exhibit a greater efficacy than capsaicin itself. These results may provide insight into the TRPV1-mediated effects of piperine on gastrointestinal function.
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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.