TRPC5 | Transient Receptor Potential Cation Channel Subfamily C Member 5
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
TRPC5: Background information
TRPC5, aslo called Short transient receptor potential channel 5 or transient receptor protein 5 is a multi-pass membrane protein and is thought to form a receptor-activated non-selective calcium permeant cation channel. The protein is active alone or as a heteromultimeric assembly with TRPC1, TRPC3, and TRPC4. TRPC5 has been implicated in the mechanism of mercury toxicity and neurological behavior
Gene:
TRPC5
Human Protein:
UniProt Q9UL62
Tissue:
Brain, adult heart, testis, ovaries
Function/ Application:
Pressure sensing, TRPC5 counteracts TRPC1 in regulating neurite outgrowth and appears to be involved in growth cone collapse that occurs when the growth cone detects a repellant factor
Pathology:
Hypertrophic Pyloric Stenosis
Interaction:
TRPC1, TRPC3, TRPC4, calmodulin, CABP1, enkurin, Na+–H exchange regulatory factor, interferon-induced GTP-binding protein, ring finger protein 24, SEC14 domain and spectrin repeat-containing protein 1, Calcium channel, voltage-dependent, gamma subunit, Mitochondrial calcium uniporter 3
Modulator:
Thioredoxin
Assays:
Patch Clamp: whole cell
Particularities:
Ligand-gated ion channel, as well as mechano-sensitive ion channel
Recommended Reviews:International Union of Pharmacology. XLVII. Nomenclature and Structure-Function Relationships of Voltage-Gated Sodium Channels. Pharmacol Rev 57: 397–409, Catterall, et al. 2005
Data and Applications
TRPC5 - Block by Gadolinium
Patchliner data and applications:
Data are taken from Milligan C.J. et al., Nature Protocols, 2009, 4(2), 244-255.
Current voltage relationships showing activaion of TRPC5 by extracellular application of Gd3+ (100 μM). Voltage ramps (−100 mV to 100 mV, holding potential 0 mV) were for 1s at 0.1 Hz.
Application Notes
TRPC5 - "Internal perfusion of Ca2+ to activate hTRPC5 on Nanion's SyncroPatch 384PE"
SyncroPatch 384PE (a predecessor model of the SyncroPatch 384) application note 
(1.7 MB)
Cells were kindly provided by Charles River.
Posters
2017 - lnvestigation of the Ion Channels hTMEM16A/Ano1 and TRPC5 and their Modulation by Intracellular Calcium
SyncroPatch 384PE (a predecessor model of the SyncroPatch 384) poster, BPS Meeting 2017 (1.3 MB)
Publications
2022 - Further Exploration of the Benzimidazole Scaffold as TRPC5 Inhibitors: Identification of 1-Alkyl-2-(pyrrolidin-1-yl)-1H-benzo[d]imidazoles as Potent and Selective Inhibitors
SyncroPatch 384PE (a predecessor model of the SyncroPatch 384 instrument) Publication in ChemMedChem (2022)
Authors:
Sharma S., Pablo J., Tolentino K., Gallegos W., Hinman J., Beninato M., Asche M., Greka A., Hopkins C.
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.
2019 - Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903
SyncroPatch 384PE (a predecessor model of SyncroPatch 384i) article in Bioorganic and Medicinal Chemistry Letters (2019)
Authors:
Sharma, S.H., Pablo J.L., Montesinos, M.S., Greka, A., Hopkins, C.R.
2011 - Rapid and Contrasting Effects of Rosiglitazone on Transient Receptor Potential TRPM3 and TRPC5 Channels
Patchliner publication in Molecular Pharmacology (2011)
Authors:
Majeed Y., Bahnasi Y., Seymour V.A.L., Wilson L.A., Milligan C.J., Agarwal A.K., Sukumar P., Naylor J., Beech D.J.
2009 - Robotic multiwell planar patch-clamp for native and primary mammalian cells
Patchliner publication in Nature Protocols (2009)
Authors:
Milligan C.J., Li J., Sukumar P., Majeed Y., Dallas M.L., English A., Emery P., Porter K.E., Smith A.M., McFadzean I., Beccano-Kelly D., Bahnasi Y., Cheong A., Naylor J., Zeng F., Liu X., Gamper N., Jiang L., Pearson H.A., Peers C., Robertson B., Beech D.J.
2008 - TRPC channel activation by extracellular thioredoxin
Patchliner publication in Nature (2008)
Authors:
Xu S.Z., Sukumar P., Zeng F., Li J., Jairaman A., English A., Naylor J., Ciurtin C., Majeed Y., Milligan C.J., Bahnasi Y.M., Al-Shawaf E., Porter K.E., Jiang L.H., Emery P., Sivaprasadarao A., Beech D.J.
2008 - Production of a specific extracellular inhibitor of TRPM3 channels
Patchliner publication in British Journal of Pharmacology (2008)
Authors:
Naylor J., Milligan C.J., Zeng F., Jones C., Beech D.J.