ArticleBiophysical journal2003
Capsaicin activation of the pain receptor, VR1: multiple open states from both partial and full binding.
Article in Biophysical journal, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 papers.
What it found
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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
58 citing papers in PubMed, 113 citations in OpenAlex.
- Permeant cations modulate pore dynamics and gating of TRPV1 ion channels.The Journal of general physiology · 2024Article
- Cannflavins isolated from Cannabis sativa impede Caenorhabditis elegans response to noxious heat.Naunyn-Schmiedeberg's archives of pharmacology · 2024Article
- Binding interactions of fatty acyl lipid mediators within the vanilloid pocket of TRPV1: A molecular dynamics study.Prostaglandins & other lipid mediators · 2023Review
- Opening of capsaicin receptor TRPV1 is stabilized equally by its four subunits.The Journal of biological chemistry · 2023Article
- Pathophysiological Roles of Transient Receptor Potential (Trp) Channels and Zinc Toxicity in Brain Disease.International journal of molecular sciences · 2023Review
- A journey from molecule to physiology andFrontiers in pharmacology · 2023Review
- Thermogenic adipose tissue in energy regulation and metabolic health.Frontiers in endocrinology · 2023Review
- The human TRPA1 intrinsic cold and heat sensitivity involves separate channel structures beyond the N-ARD domain.Nature communications · 2022Article
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- Vanilloid-dependent TRPV1 opening trajectory from cryoEM ensemble analysis.Nature communications · 2022Article
- TRPV1 in arteries enables a rapid myogenic tone.The Journal of physiology · 2022Article
- Article
- Functional evidence of distinct electrophile-induced activation states of the ion channel TRPA1.Biochemistry and biophysics reports · 2021Article
- TRPV1 Channel Activated by the PGE2/EP4 Pathway Mediates Spinal Hypersensitivity in a Mouse Model of Vertebral Endplate Degeneration.Oxidative medicine and cellular longevity · 2021Article
- TRPV1 expressed throughout the arterial circulation regulates vasoconstriction and blood pressure.The Journal of physiology · 2020Article
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- Structural mechanisms of transient receptor potential ion channels.The Journal of general physiology · 2020Review
- TRPV1 Tunes Optic Nerve Axon Excitability in Glaucoma.Frontiers in physiology · 2020Article
- Mammalian TRP ion channels are insensitive to membrane stretch.Journal of cell science · 2019Article
- Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Capsaicin, the pungent ingredient of hot peppers, has long been used to identify nociceptors. Its molecular target, the vanilloid receptor VR1, was recently cloned and confirmed functionally as a polymodal detector of multiple pain stimuli: heat, acid, and vanilloids. Previous electrophysiology studies have focused on whole-cell characteristics of the receptor. Here, we provide the first in-depth single-channel kinetic study of VR1 to understand its activation mechanism. At low to medium concentrations, channel activity appeared as bursts. Not only did the durations of the interburst gaps vary with capsaicin, the bursts also appeared ligand-dependent, with high capsaicin prolonging bursts and stabilizing openings. Gating involved at least five closed and three open states, with strong correlations between short closures and long openings, and long closures and short openings. Increasing capsaicin reduced the long closures with little effect on short ones. The open time constants changed little with capsaicin concentration, though their relative proportions varied. These results suggest that 1), the channel contains multiple capsaicin binding sites; 2), both partial and full binding are capable of opening the channel; 3), when activated, multiple open states are accessible irrespective of the level of binding; and 4), capsaicin association occurs preferentially to the closed channel.
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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.