ArticleBiophysical journal2007
On the mechanism of TBA block of the TRPV1 channel.
Article in Biophysical journal, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 44 citations in OpenAlex.
- Decoding Pancreatic Cancer Pain: From Tumor-Nerve Crosstalk to Targeted Analgesic Strategies.International journal of medical sciences · 2026Review
- Structural basis of the inhibition of TRPV1 by analgesic sesquiterpenes.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Identification and Properties of TRPV4 Mutant Channels Present in Polycystic Kidney Disease Patients.Function (Oxford, England) · 2024Article
- NGF-mediated crosstalk: unraveling the influence of metabolic deregulation on the interplay between neural and pancreatic cancer cells and its impact on patient outcomes.Frontiers in pharmacology · 2024Review
- Asymmetric Interplay Between KFrontiers in physiology · 2021Article
- Article
- Structural mechanisms of transient receptor potential ion channels.The Journal of general physiology · 2020Review
- Article
- Different agonists induce distinct single-channel conductance states in TRPV1 channels.The Journal of general physiology · 2018Article
- Article
- Article
- The role of endogenous molecules in modulating pain through transient receptor potential vanilloid 1 (TRPV1).The Journal of physiology · 2013Review
- Permeation and block of TRPV1 channels by the cationic lidocaine derivative QX-314.Journal of neurophysiology · 2013Article
- Antioncogenic effects of transient receptor potential vanilloid 1 in the progression of transitional urothelial cancer of human bladder.ISRN urology · 2012Article
- Targeting of sodium channel blockers into nociceptors to produce long-duration analgesia: a systematic study and review.British journal of pharmacology · 2011Article
- Identification of a binding motif in the S5 helix that confers cholesterol sensitivity to the TRPV1 ion channel.The Journal of biological chemistry · 2011Article
- Nobilamides A-H, long-acting transient receptor potential vanilloid-1 (TRPV1) antagonists from mollusk-associated bacteria.Journal of medicinal chemistry · 2011Article
- Biological physics in México: Review and new challenges.Journal of biological physics · 2011Article
- Moving towards supraspinal TRPV1 receptors for chronic pain relief.Molecular pain · 2010Review
- Intrinsic versus extrinsic voltage sensitivity of blocker interaction with an ion channel pore.The Journal of general physiology · 2010Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The transient receptor potential vanilloid 1 (TRPV1) channel is a nonselective cation channel activated by capsaicin and responsible for thermosensation. To date, little is known about the gating characteristics of these channels. Here we used tetrabutylammonium (TBA) to determine whether this molecule behaves as an ion conduction blocker in TRPV1 channels and to gain insight into the nature of the activation gate of this protein. TBA belongs to a family of classic potassium channel blockers that have been widely used as tools for determining the localization of the activation gate and the properties of the pore of several ion channels. We found TBA to be a voltage-dependent pore blocker and that the properties of block are consistent with an open-state blocker, with the TBA molecule binding to multiple open states, each with different blocker affinities. Kinetics of channel closure and burst-length analysis in the presence of blocker are consistent with a state-dependent blocking mechanism, with TBA interfering with closing of an activation gate. This activation gate may be located cytoplasmically with respect to the binding site of TBA ions, similar to what has been observed in potassium channels. We propose an allosteric model for TRPV1 activation and block by TBA, which explains our experimental data.
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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.