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
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
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
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.
TRPM8 / TRPV1 - Pharmacology
Port-a-Patch data and applications:
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
2021 - Activation and inhibition of assay-ready TRPA1 and TRPV cells: an automated patch clamp study
Port-a-Patch, 
Patchliner and 
SyncroPatch 384i (a predecessor model of SyncroPatch 384) Biophysical Society Meeting 2021 
(1.5MB)
2016 - Next level toxicity screening: From single channel to overall cell behavior
Orbit mini, 
CardioExcyte 96 and 
SyncroPatch 384PE (a predecessor model of the SyncroPatch 384) poster, Meeting of the French Society of Toxinology (SFET) 2015 (0.9 MB)
2015 - The backstage pass to study your favorite TRP channel
Port-a-Patch and Patchliner and SyncroPatch 384PE (a predecessor model of the SyncroPatch 384) poster, TRP Meeting 2015 (2.2 MB)
Webinars
28.04.2020 | Webinar: Validation and optimization of automated patch clamp voltage-gated Ca2+ channel assays
Patchliner Webinar
Date: April 28. 2020, 4:00 PM CET (10:00 AM EDT)
Marc will outline the development, optimization and validation of a range of voltage-gated Ca2+ channel assays on the Patchliner automated patch clamp platform that were subsequently used in an 8 year drug discovery collaboration between Metrion Biosciences and a german pharma company.
Speakers:
Dr. Marc Rogers (Chief Scientific Officer, Metrion Biosciences)
Dr. András Horváth (Application Scientist, Nanion Technologies)
27.01.2016 | Webinar: Instant bilayers - just add protein
Orbit 16 and Orbit Mini
This 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
TRPV1 - "Temperature activation of TRPV1 reconstituted into planar lipid bilayers and recorded using the Orbit mini platform"
Orbit mini application note (0.4 MB)
TRPV1 - "Heat activation of TRPV1 on Nanion's Patchliner"
Patchliner application note: (0.5 MB)
TRPM8 / TRPV1 - "TRPV1 and TRPM8 recorded on Nanion's Port-a-Patch"
Port-a-Patch application note: (0.2 MB)
Publications
2021 - L-carnitine suppresses transient receptor potential vanilloid type 1 activity and myofibroblast transdifferentiation in human corneal keratocytes
Port-a-Patch Publication in Lab Invest (2021)
Authors:
Turan E., Valtink M., Reinach P.S., Skupin A., Luo H., Brockmann T., Salem M.H.O.B., Pleyer U., Mergler S.
2021 - High-Throughput Screening of TRPV1 Ligands in the Light of the Bioluminescence Resonance Energy Transfer Technique
SyncroPatch 384 Publication in Molecular Pharmacology (2021)
Authors:
Chappe Y., Michel P., Joushomme A., Barbeau S., Pierredon S., Baron L., Garenne A., Poulletier De Gannes F., Hurtier A., Mayer S., Lagroye I., Quignard J-F., Ducret T., Compan V., Franchet C., Percherancier Y.
2019 - Purification of Functional Human TRP Channels Recombinantly Produced in Yeast
Orbit mini publication in Cells (2019)
Authors:
Zhang L., Wang K., Klaerke D.A., Calloe K., Lowrey L., Pedersen P.A., Gourdon P., Gotfryd K.
2018 - Vascular Endothelial Growth Factor (VEGF) Induced Downstream Responses to Transient Receptor Potential Vanilloid 1 (TRPV1) and 3-Iodothyronamine (3-T1AM) in Human Corneal Keratocytes
Port-a-Patch publication in Frontiers in Pharmacology (2018)
Authors:
Türker, E., Garreis, F., Khajavi, N., Reinach, P.S., Joshi, P., Brockmann, T., Lucius, A., Ljubojevic, N., Turan, E., Cooper, D., Schick, F., Reinholz, R., Pleyer, U., Köhrle, J., Mergler, S.
2018 - TRPM8 Activation via 3-Iodothyronamine Blunts VEGF-Induced Transactivation of TRPV1 in Human Uveal Melanoma Cells
Port-a-Patch publication in Frontiers in Pharmacology (2018)
Authors:
Walcher, L., Budde, C., Böhm, A., Reinach, P.S., Dhandapani, P., Ljubojevic, N., Schweiger, M.W., von der Waydbrink, H., Reimers, I., Köhrle, J., Mergler, S.
2016 - Upregulation of Transient Receptor Potential Vanilloid Type-1 Channel Activity and Ca2+ Influx Dysfunction in Human Pterygial Cells
Port-a-Patch publication in Investigative Opthalmology & Visual Science (2016)
Authors:
Garreis F., Schröder A., Reinach P.S., Zoll S., Khajavi N., Dhandapani P., Lucius A., Pleyer U., Paulsen F., Mergler S.
2016 - Photosensitization in Porphyrias and Photodynamic Therapy Involves TRPA1 and TRPV1
Port-a-Patch and 
Vesicle Prep Pro publication in The Journal of Neuroscience (2016)
Authors:
Babes A., Sauer S.K., Moparthi L., Kichko T.I., Neacsu C., Namer B., Filipovic M., Zygmunt P.M., Reeh P.W., Fischer M.J.
2014 - L-Carnitine Reduces in Human Conjunctival Epithelial Cells Hypertonic- Induced Shrinkage through Interacting with TRPV1 Channels
Port-a-Patch publication in Cellular Physiology and Biochemistry (2014)
Authors:
Khajavi N., Reinach P.S., Skrzypski M., LudeA., Mergler S.
2014 - Calcium regulation by temperature-sensitive transient receptor potential channels in human uveal melanoma cells
Port-a-Patch publication in Cellular Signalling (2014)
Authors:
Mergler S., Derckx R., Reinach P.S., Garreis F., Böhm A., Schmelzer L., Skosyrski S., Ramesh N., Abdelmessih S., Polat O.K., Khajavi N., Riechardt A.I.
2013 - Monoacylglycerols Activate TRPV1 – A Link between Phospholipase C and TRPV1
Port-a-Patch publication in PLoS One (2013)
Authors:
Zygmunt P.M., Ermund A., Movahed P., Andersson D.A., Simonsen C., Jönsson B.A., Blomgren A., Birnir B., Bevan S., Eschalier A., Mallet C., Gomis A., Högestätt E.D.
2012 - Thermo-sensitive transient receptor potential vanilloid channel-1 regulates intracellular calcium and triggers chromogranin A secretion in pancreatic neuroendocrine BON-1 tumor cells
Port-a-Patch publication in Cellular Signalling (2012)
Authors:
Mergler S., Skrzypski M., Sassek M., Pietrzak P., Pucci C., Wiedenmann B., Strowski M.Z.
2012 - Insulin-secreting INS-1E cells express functional TRPV1 channels
Port-a-Patch publication in Islets (2012)
Authors:
Fågelskiöld A.J., Kannisto K., Boström A., Hadrovic B., Farre C., Eweida M., Wester K., Islam MD.S.
2012 - Calcium regulation by thermo- and osmosensing transient receptor potential vanilloid channels (TRPVs) in human conjunctival epithelial cells
Port-a-Patch publication in Histochemistry and Cell Biology (2012)
Authors:
Mergler S., Garreis F., Sahlmüller M., Lyras E.-M., Reinach P.S., Dwarakanath A., Paulsen F., Pleyer U.
2011 - Thermosensitive transient receptor potential channels in human corneal epithelial cells
Port-a-Patch publication in Journal of Cellular Physiology (2011)
Authors:
Mergler S., Garreis F., Sahlmüller M., Reinach P.S., Paulsen F., and Pleyer U.
2011 - Physiology of the Human Corneal Endothelium – New Insights from Electrophysiological Investigations
Port-a-Patch publication in Klinische Monatsblätter für Augenheilkunde (2011)
Authors:
Mergler S. and Pleyer U.
2011 - The Chimeric approach reveals that differences in the TRPV1 pore domain determine species-specific sensitivity to block of heat activation
Patchliner publication in Journal of Biological Chemistry (2011)
Authors:
Papakosta M., Dalle C., Haythornthwaite A., Cao L., Stevens E.B., Burgess G., Russell R., Cox P.J., Phillips S.C., Grimm C.
2010 - TRPV channels mediate temperature-sensing in human corneal endothelial cells
Port-a-Patch publication in Experimental Eye Research (2010)
Authors:
Mergler S., Valtink M., Coulson-Thomas V.J., Lindemann D., Reinach P.S., Engelmann K., Pleyer U.
2009 - Port-a-Patch and Patchliner: High fidelity electrophysiology for secondary screening and safety pharmacology
Port-a-Patch and Patchliner publication in Combinatorial Chemistry & High Throughput Screening (2009)
Authors:
Farre C., Haythornthwaite A., Haarmann C., Stoelzle S., Kreir M., George M., Brüggemann A., Fertig N.