TRPV1 | Transient Receptor Potential Cation Channel Subfamily V Member 1

Family:
Transient  receptor potential channels

Subgroups:
TRPC (TRPC1–TRPC7), TRPV (TRPV1-TRPV6), TRPA1, TRPM (TRPM1–TRPM8), TRPP (TRPP1–TRPP3, PKD1, PKDREJ, PKDL1–PKDL3), TRPML (TRPML1–TRPML3), TRPN

Topology:
Most TRP channels are composed of 6 transmembrane domains (helices) with intracellular N- and C-termini, non-selectively permeable to various cations

TRPV1: Background information

TRPV1, also known as capsaicin receptor and vanilloid receptor 1, was the first isolated member of the transient receptor potential vanilloid receptor proteins. The function of TRPV1 is detection and regulation of body temperature. In addition, TRPV1 provides a sensation of scalding heat and pain (nociception). TRPV1 may be activated by a wide variety of exogenous and endogenous physical and chemical stimuli. The best-known activators of TRPV1 are: temperature greater than 43 °C (109 °F); acidic conditions; capsaicin, the irritating compound in hot chili peppers. Upon prolonged exposure to capsaicin, TRPV1 activity decreases, a phenomenon called desensitization. Extracellular calcium ions are required for this phenomenon, thus influx of calcium and the consequential increase of intracellular calcium mediate this effect.

Gene:
TRPV1

Human Protein:
UniProt Q8NER1

Tissue:
Nociceptors, sensory neurons, brain, skin

Function/ Application:
Noxious chemical and thermal stimuli reception, apoptosis, temperature transducer for ‘‘heat’’

Pathology:
Pain, incontinence, inflammation, thermoception

Interaction:
TRPV2, TRPV3, calmodulin, PI3 kinase, PRKCE, PRKCM, adenosine

Modulator:
Capsaicin, alpha-linolenic acid, reiniferatoxin, vanillotoxin, agatoxin 489, capsazepine

Particularities:
Ligand-gated ion channel, as well as temperature- and pH-sensitive ion channel.

Assays:
Patch Clamp: whole cell, intracellular perfusion, temperature control;
Bilayer recordings: Temperature control

Recommended Reviews:
International Union of Pharmacology. XLIII. Compendium of voltage-gated ion channels: transient receptor potential channels., Pharmacol Rev 55(4):591-6 Clapham, et al. 2003 

Data and Applications

TRPV1 - Transient Heat Activation

p36 2 TRPV1icon pl   Patchliner data and applications:

The current responses of a CHO cell expressing TRPV1 (ramp -100 mV to +100 mV) at increasing temperatures is shown. The ET50 value was determined as 64°C. Challenge of the same cell with capsaicin (1 μM) and temperature (70°C) allows comparison of the responses. IC50s for ruthenium red block of capsaicin- and heat-responses were determined as 1.6 ± 0.2 μM (n = 3) and 7.4 ± 1.3 μM (n = 3), respectively.

TRPV1 - Heat Activation

p28 2 heatActivChanicon pap   Port-a-Patch data and applications:

Raw traces of TRPV1 current responses to voltage ramps from –100 mV up to +100 mV. TRPV1 current at RT (28°C), during two stimulations by application of heated solution (34°C and 36°C), and after cooling down to RT (29°C). The picture on the right-hand side shows the current amplitudes as recorded at -100 mV and +100 mV plotted against time.

TRPV1 - External Perfusion of Capsaicin

application trpv1 1icon pap   Port-a-Patch data and applications:
Data were kindly provided by David Cohen, Oregon Health & Science University, Portland, USA.

Whole cell current responses from HEK 293 cells transiently expressing TRPV1 to a ramp voltage protocol (‑100 mV to +100 mV). Capsaicin at a concentration of 2 μM reversibly activated the channel.

TRPV1 - Application of Capsaicin

TRPV1 bea verzerrticon sp96   SyncroPatch 96 (a predecessor model of SyncroPatch 384PE) data and applications:

Using the SyncroPatch 96 CHO cells expressing TRPV1 were subjected to a voltage ramp (-100 mV to +100 mV) in the presence and absence (control) of 2 μM capsaicin. As shown in the exemplar traces, inward and outward currents increase upon capsaicin addition.

TRPV1 - Activation by Internal Application of Capsaicin

0TRPV1 Internal Acticon sp96   SyncroPatch 96 (a predecessor model of SyncroPatch 384PE) data and applications:

The SyncroPatch 96 allows continues recording during the application of compounds from the intracellular side. Here, TRPV1 channels were activated by the internal application of capsaicin.

   

 

 

 

TRPM8 / TRPV1 - Pharmacology

icon pap   Port-a-Patch data and applications:p15 1 TRP 
TRPV1 data were kindly supplied by Dr. David Cohen, Oregon Health and Service University, Portland, OR, USA.

TRP channels recorded in HEK293 cells. Menthol (dark blue) activated the TRPM8 channels (shown on the left) and could be inhibited by genistein (blue). TRPV1 channels expressed in HEK293 cells (right) were stimulated by application of capsaicin.

Posters

2016 - Next level toxicity screening: From single channel to overall cell behavior

Icon Orbit Mini   Orbit mini,   Icon CE   CardioExcyte 96 and   icon sp96   SyncroPatch 384PE poster, Meeting of the French Society of Toxinology (SFET) 2015  logo pdf   (0.9 MB)

2015 - "The backstage pass to study your favorite TRP channel"

icon pap   Port-a-Patch and   icon pl   Patchliner and SyncroPatch 384PE and   icon sp96   SyncroPatch 384PE poster, TRP Meeting 2015   logo pdf   (2.2 MB)

Webinars

27.01.2016 | Webinar: Instant bilayers - just add protein.

Icon Orbit   Orbit 16 and   Icon Orbit Mini   Orbit Mini

Orbits V1 flat 250pxThis webinar covers the use of the lipid bilayer platforms from Nanion: the Orbit16 and the Orbit mini for characterization of membrane proteins like ion channels, bacterial porins and biological nanopores. Both bilayer systems support high quality low noise recordings, but differ in throughput capabilities and experimental features. The Orbit16, introduced in 2012 is a device for efficient formation of 16 lipid bilayers simultaneously, allowing for parallel bilayer-reconstitution of ion channels and nanopores.

 

Application Notes

Publications

2016 - Upregulation of Transient Receptor Potential Vanilloid Type-1 Channel Activity and Ca2+ Influx Dysfunction in Human Pterygial Cells

icon pap  Port-a-Patch publication in Investigative Opthalmology & Visual Science (2016)

2016 - Photosensitization in Porphyrias and Photodynamic Therapy Involves TRPA1 and TRPV1

icon pap  Port-a-Patch and   icon vpp   Vesicle Prep Pro publication in The Journal of Neuroscience (2016)

2014 - L-Carnitine Reduces in Human Conjunctival Epithelial Cells Hypertonic- Induced Shrinkage through Interacting with TRPV1 Channels

icon pap  Port-a-Patch publication in Cellular Physiology and Biochemistry (2014)

2014 - Calcium regulation by temperature-sensitive transient receptor potential channels in human uveal melanoma cells

icon pap  Port-a-Patch publication in Cellular Signalling (2014)

2013 - Monoacylglycerols Activate TRPV1 – A Link between Phospholipase C and TRPV1

icon pap   Port-a-Patch publication in PLoS One (2013)

2012 - Thermo-sensitive transient receptor potential vanilloid channel-1 regulates intracellular calcium and triggers chromogranin A secretion in pancreatic neuroendocrine BON-1 tumor cells

icon pap   Port-a-Patch publication in Cellular Signalling (2012)

2012 - Insulin-secreting INS-1E cells express functional TRPV1 channels

icon pap   Port-a-Patch publication in Islets (2012)

2012 - Calcium regulation by thermo- and osmosensing transient receptor potential vanilloid channels (TRPVs) in human conjunctival epithelial cells

icon pap   Port-a-Patch publication in Histochemistry and Cell Biology (2012)

2011 - Thermosensitive transient receptor potential channels in human corneal epithelial cells

icon pap   Port-a-Patch publication in Journal of Cellular Physiology (2011)

2011 - Physiology of the Human Corneal Endothelium – New Insights from Electrophysiological Investigations

icon pap   Port-a-Patch publication in Klinische Monatsblätter für Augenheilkunde (2011)

2011 - The Chimeric approach reveals that differences in the TRPV1 pore domain determine species-specific sensitivity to block of heat activation

icon pl   Patchliner publication in Journal of Biological Chemistry (2011)

2010 - TRPV channels mediate temperature-sensing in human corneal endothelial cells

icon pap  Port-a-Patch publication in Experimental Eye Research (2010)

2009 - Port-a-Patch and Patchliner: High fidelity electrophysiology for secondary screening and safety pharmacology

icon pap  Port-a-Patch and   icon pl   Patchliner publication in Combinatorial Chemistry & High Throughput Screening (2009)

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