Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Biophys J
2003 Nov 01;855:2988-3006. doi: 10.1016/S0006-3495(03)74719-5.
Show Gene links
Show Anatomy links
Thermodynamics of heat activation of single capsaicin ion channels VR1.
Liu B
,
Hui K
,
Qin F
.
???displayArticle.abstract???
Temperature affects functions of all ion channels, but few of them can be gated directly. The vanilloid receptor VR1 provides one exception. As a pain receptor, it is activated by heat >42 degrees C in addition to other noxious stimuli, e.g. acids and vanilloids. Although it is understood how ligand- and voltage-gated channels might detect their stimuli, little is known on how heat could be sensed and activate a channel. In this study, we characterized the heat-induced single-channel activity of VR1, in an attempt to localize the temperature-dependent components involved in the activation of the channel. At <42 degrees C, openings were few and brief. Raising the ambient temperature rapidly increased the frequency of openings. Despite the large temperature coefficient of the apparent activity (Q(10) approximately 27), the unitary current, the open dwell-times, and the intraburst closures were all only weakly temperature dependent (Q(10) < 2). Instead, heat had a localized effect on the reduction of long closures between bursts (Q(10) approximately 7) and the elongation of burst durations (Q(10) approximately 32). Both membrane lipids and solution ionic strength affected the temperature threshold of the activation, but neither diminished the response. The thermodynamic basis of heat activation is discussed, to elucidate what makes a thermal-sensitive channel unique.
Anderson,
Potential-dependent transition temperature of ionic channels induced by glutamate in locust muscle.
1977, Pubmed
Anderson,
Potential-dependent transition temperature of ionic channels induced by glutamate in locust muscle.
1977,
Pubmed
Beam,
A quantitative study of potassium channel kinetics in rat skeletal muscle from 1 to 37 degrees C.
1983,
Pubmed
Boheim,
Charge-pulse relaxation studies with lipid bilayer membranes modified by alamethicin.
1978,
Pubmed
Bolotina,
Variations of membrane cholesterol alter the kinetics of Ca2(+)-dependent K+ channels and membrane fluidity in vascular smooth muscle cells.
1989,
Pubmed
Caterina,
A capsaicin-receptor homologue with a high threshold for noxious heat.
1999,
Pubmed
,
Xenbase
Caterina,
The capsaicin receptor: a heat-activated ion channel in the pain pathway.
1997,
Pubmed
,
Xenbase
Cesare,
A novel heat-activated current in nociceptive neurons and its sensitization by bradykinin.
1996,
Pubmed
Chang,
Attenuation of channel kinetics and conductance by cholesterol: an interpretation using structural stress as a unifying concept.
1995,
Pubmed
Chiu,
Anomalous temperature dependence of the sodium conductance in rabbit nerve compared with frog nerve.
1979,
Pubmed
Christian,
Use of cyclodextrins for manipulating cellular cholesterol content.
1997,
Pubmed
DeCoursey,
Temperature dependence of voltage-gated H+ currents in human neutrophils, rat alveolar epithelial cells, and mammalian phagocytes.
1998,
Pubmed
García-Martínez,
Identification of an aspartic residue in the P-loop of the vanilloid receptor that modulates pore properties.
2000,
Pubmed
,
Xenbase
Gleason,
Excess membrane cholesterol alters calcium movements, cytosolic calcium levels, and membrane fluidity in arterial smooth muscle cells.
1991,
Pubmed
Gunthorpe,
The diversity in the vanilloid (TRPV) receptor family of ion channels.
2002,
Pubmed
Güler,
Heat-evoked activation of the ion channel, TRPV4.
2002,
Pubmed
,
Xenbase
Hui,
Capsaicin activation of the pain receptor, VR1: multiple open states from both partial and full binding.
2003,
Pubmed
,
Xenbase
Jancsó,
Direct evidence for neurogenic inflammation and its prevention by denervation and by pretreatment with capsaicin.
1967,
Pubmed
Jordt,
Molecular basis for species-specific sensitivity to "hot" chili peppers.
2002,
Pubmed
Jordt,
Acid potentiation of the capsaicin receptor determined by a key extracellular site.
2000,
Pubmed
Julius,
Molecular mechanisms of nociception.
2001,
Pubmed
Jung,
Agonist recognition sites in the cytosolic tails of vanilloid receptor 1.
2002,
Pubmed
,
Xenbase
Jung,
Capsaicin binds to the intracellular domain of the capsaicin-activated ion channel.
1999,
Pubmed
Jurman,
Visual identification of individual transfected cells for electrophysiology using antibody-coated beads.
1994,
Pubmed
Kirsch,
Temperature dependence of Na currents in rabbit and frog muscle membranes.
1987,
Pubmed
Kuzhikandathil,
Functional analysis of capsaicin receptor (vanilloid receptor subtype 1) multimerization and agonist responsiveness using a dominant negative mutation.
2001,
Pubmed
Kwak,
Intracellular ATP increases capsaicin-activated channel activity by interacting with nucleotide-binding domains.
2000,
Pubmed
,
Xenbase
Lee,
Temperature dependence of K(+)-channel properties in human T lymphocytes.
1990,
Pubmed
Levitan,
Membrane cholesterol content modulates activation of volume-regulated anion current in bovine endothelial cells.
2000,
Pubmed
Lundbaek,
Membrane stiffness and channel function.
1996,
Pubmed
McKemy,
Identification of a cold receptor reveals a general role for TRP channels in thermosensation.
2002,
Pubmed
,
Xenbase
Milburn,
The temperature dependence of conductance of the sodium channel: implications for mechanisms of ion permeation.
1995,
Pubmed
Montell,
A unified nomenclature for the superfamily of TRP cation channels.
2002,
Pubmed
Murrell-Lagnado,
Energetics of Shaker K channels block by inactivation peptides.
1993,
Pubmed
,
Xenbase
Nagy,
Similarities and differences between the responses of rat sensory neurons to noxious heat and capsaicin.
1999,
Pubmed
Nobile,
Fast inactivation of Shaker K+ channels is highly temperature dependent.
1997,
Pubmed
,
Xenbase
Numazaki,
Direct phosphorylation of capsaicin receptor VR1 by protein kinase Cepsilon and identification of two target serine residues.
2002,
Pubmed
Pace,
Forces contributing to the conformational stability of proteins.
1996,
Pubmed
Peier,
A TRP channel that senses cold stimuli and menthol.
2002,
Pubmed
Peier,
A heat-sensitive TRP channel expressed in keratinocytes.
2002,
Pubmed
Privalov,
Stability of proteins: small globular proteins.
1979,
Pubmed
Pusch,
Temperature dependence of fast and slow gating relaxations of ClC-0 chloride channels.
1997,
Pubmed
,
Xenbase
Qin,
Estimating single-channel kinetic parameters from idealized patch-clamp data containing missed events.
1996,
Pubmed
,
Xenbase
Qin,
Maximum likelihood estimation of aggregated Markov processes.
1997,
Pubmed
Quartararo,
Ion permeation through single ACh-activated channels in denervated adult toad sartorius skeletal muscle fibres: effect of temperature.
1988,
Pubmed
Ryu,
Low pH potentiates both capsaicin binding and channel gating of VR1 receptors.
2003,
Pubmed
Santiago,
Probing the effects of membrane cholesterol in the Torpedo californica acetylcholine receptor and the novel lipid-exposed mutation alpha C418W in Xenopus oocytes.
2001,
Pubmed
,
Xenbase
Sen,
Cholesterol increases the L-type voltage-sensitive calcium channel current in arterial smooth muscle cells.
1992,
Pubmed
Smith,
TRPV3 is a temperature-sensitive vanilloid receptor-like protein.
2002,
Pubmed
Story,
ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures.
2003,
Pubmed
Szallasi,
Vanilloid (Capsaicin) receptors and mechanisms.
1999,
Pubmed
Tominaga,
The cloned capsaicin receptor integrates multiple pain-producing stimuli.
1998,
Pubmed
,
Xenbase
Urry,
Temperature dependence of single channel currents and the peptide libration mechanism for ion transport through the gramicidin A transmembrane channel.
1984,
Pubmed
Vlachová,
The effects of capsaicin and acidity on currents generated by noxious heat in cultured neonatal rat dorsal root ganglion neurones.
2001,
Pubmed
Vlachová,
Functional role of C-terminal cytoplasmic tail of rat vanilloid receptor 1.
2003,
Pubmed
Vyklický,
Temperature coefficient of membrane currents induced by noxious heat in sensory neurones in the rat.
1999,
Pubmed
Welch,
The activation mechanism of rat vanilloid receptor 1 by capsaicin involves the pore domain and differs from the activation by either acid or heat.
2000,
Pubmed
,
Xenbase
Xu,
TRPV3 is a calcium-permeable temperature-sensitive cation channel.
2002,
Pubmed
Yang,
Folding at the speed limit.
2003,
Pubmed
Yeagle,
Cholesterol and the cell membrane.
1985,
Pubmed
