ArticleThe Journal of general physiology2008
Properties of the inner pore region of TRPV1 channels revealed by block with quaternary ammoniums.
Article in The Journal of general physiology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 40 citations in OpenAlex.
- Identifying targets to prevent aminoglycoside ototoxicity.Molecular and cellular neurosciences · 2022Review
- In vivo real-time imaging reveals megalin as the aminoglycoside gentamicin transporter into cochlea whose inhibition is otoprotective.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Article
- Systemic Fluorescent Gentamicin Enters Neonatal Mouse Hair Cells Predominantly Through Sensory Mechanoelectrical Transduction Channels.Journal of the Association for Research in Otolaryngology : JARO · 2020Article
- Article
- Inflammation up-regulates cochlear expression of TRPV1 to potentiate drug-induced hearing loss.Science advances · 2019Article
- Insulin Release Mechanism Modulated by Toxins Isolated from Animal Venoms: From Basic Research to Drug Development Prospects.Molecules (Basel, Switzerland) · 2019Review
- Different agonists induce distinct single-channel conductance states in TRPV1 channels.The Journal of general physiology · 2018Article
- Aminoglycoside-Induced Cochleotoxicity: A Review.Frontiers in cellular neuroscience · 2017Review
- Potential Mechanisms Underlying Inflammation-Enhanced Aminoglycoside-Induced Cochleotoxicity.Frontiers in cellular neuroscience · 2017Review
- Lactate is a potent inhibitor of the capsaicin receptor TRPV1.Scientific reports · 2016Article
- Rhodamine analogues for molecular ruler applications.Dyes and pigments : an international journal · 2016Article
- Structural biology of TRP channels.Handbook of experimental pharmacology · 2014Review
- Coarse architecture of the transient receptor potential vanilloid 1 (TRPV1) ion channel determined by fluorescence resonance energy transfer.The Journal of biological chemistry · 2013Article
- Permeation and block of TRPV1 channels by the cationic lidocaine derivative QX-314.Journal of neurophysiology · 2013Article
- Bumetanide hyperpolarizes madin-darby canine kidney cells and enhances cellular gentamicin uptake by elevating cytosolic Ca(2+) thus facilitating intermediate conductance Ca(2+)--activated potassium channels.Cell biochemistry and biophysics · 2013Article
- Exploring structure-function relationships between TRP and Kv channels.Scientific reports · 2013Article
- Voltage-dependent gating in a "voltage sensor-less" ion channel.PLoS biology · 2010Article
- The 63rd Symposium of the Society of General Physiologists: "muscles" instead of squid at Woods Hole.The Journal of general physiology · 2009Article
- Structural determinants of gating in the TRPV1 channel.Nature structural & molecular biology · 2009Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The transient receptor potential vanilloid 1 (TRPV1) nonselective cationic channel is a polymodal receptor that activates in response to a wide variety of stimuli. To date, little structural information about this channel is available. Here, we used quaternary ammonium ions (QAs) of different sizes in an effort to gain some insight into the nature and dimensions of the pore of TRPV1. We found that all four QAs used, tetraethylammonium (TEA), tetrapropylammonium (TPrA), tetrabutylammonium, and tetrapentylammonium, block the TRPV1 channel from the intracellular face of the channel in a voltage-dependent manner, and that block by these molecules occurs with different kinetics, with the bigger molecules becoming slower blockers. We also found that TPrA and the larger QAs can only block the channel in the open state, and that they interfere with the channel's activation gate upon closing, which is observed as a slowing of tail current kinetics. TEA does not interfere with the activation gate, indicating that this molecule can reside in its blocking site even when the channel is closed. The dependence of the rate constants on the size of the blocker suggests a size of around 10 A for the inner pore of TRPV1 channels.
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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.