Gene and Protein Information
Species	TM	P Loops	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	6	0	1119	8q21.11	TRPA1	transient receptor potential cation channel subfamily A member 1	63
Mouse	6	0	1125	1 A3	Trpa1	transient receptor potential cation channel, subfamily A, member 1	131
Rat	6	0	1125	5q11	Trpa1	transient receptor potential cation channel, subfamily A, member 1	64

Previous and Unofficial Names

ANKTM1 | TRPN1 | ankyrin-like with transmembrane domains 1 | transient receptor potential cation channel

Database Links
Alphafold	O75762 (Hs), Q8BLA8 (Mm), Q6RI86 (Rn)
CATH/Gene3D	1.25.40.20
ChEMBL Target	CHEMBL6007 (Hs), CHEMBL1075310 (Mm), CHEMBL5160 (Rn)
DrugBank Target	O75762 (Hs)
Ensembl Gene	ENSG00000104321 (Hs), ENSMUSG00000032769 (Mm), ENSRNOG00000007354 (Rn)
Entrez Gene	8989 (Hs), 277328 (Mm), 312896 (Rn)
Human Protein Atlas	ENSG00000104321 (Hs)
KEGG Gene	hsa:8989 (Hs), mmu:277328 (Mm), rno:312896 (Rn)
OMIM	604775 (Hs)
Pharos	O75762 (Hs)
RefSeq Nucleotide	NM_007332 (Hs), NM_177781 (Mm), NM_207608 (Rn)
RefSeq Protein	NP_015628 (Hs), NP_808449 (Mm), NP_997491 (Rn)
UniProtKB	O75762 (Hs), Q8BLA8 (Mm), Q6RI86 (Rn)
Wikipedia	TRPA1 (Hs)

Functional Characteristics
γ = 87–100 pS; conducts mono- and di-valent cations non-selectively (PCa/PNa = 0.84); outward rectification; activated by elevated intracellular Ca2+

Ion Selectivity and Conductance
Species:  Mouse Rank order:  Ca2+ = Na+ > Mg2+ References:  98
Ion Selectivity and Conductance Comments
TRPA1 exhibits conductance of 98pS in physiological solution, dependent on Ca2+ and Mg2+ concentration [98].

Voltage Dependence Comments

Voltage-dependence not yet described, inactivation by extracellular Ca2+ might be voltage dependent [98].

Chemical activators (Human)

Isothiocyanates (covalent) and 1,4-dihydropyridines (non-covalent)

Oxidative stress compounds (Mouse)

4-oxo-nonenal: pEC50 5.7, H2O2 : pEC50 3.6, hypochlorite: EC50 11 ppm (human) and 7 ppm (mouse)  [3,20,123]

Physical activators (Human)

Cooling (<17°C) (disputed)  [64,98,146]

Download all structure-activity data for this target as a CSV file

Activators
Key to terms and symbols	View all chemical structures	Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Holding voltage (mV) Reference eugenol Mm Agonist - - 6x10-4 Physiological 9 ⤷ Conc range: 6x10-4 M [9] Holding voltage: Physiological gingerol Mm Agonist - - 6x10-4 Physiological 9 ⤷ Conc range: 6x10-4 M [9] Holding voltage: Physiological methyl salicylate Mm Agonist - - 6x10-4 Physiological 9 ⤷ Conc range: 6x10-4 M [9] Holding voltage: Physiological icilin Mm Agonist - - 1x10-4 Physiological 131 ⤷ Conc range: 1x10-4 M non-covalent [131] Holding voltage: Physiological JT010 Hs Activation 9.2 pEC50 - - 135 ⤷ pEC50 9.2 (EC50 6.5x10-10 M) [135] Description: Ligand-induced calcium influx in TRPA1-transfected HEK293 cells. PF-4840154 Hs Activation 7.6 pEC50 - - 121 ⤷ pEC50 7.6 (EC50 2.51x10-8 M) This compound has similar activity at rat and mouse TRPA1 [121] Description: Calcium imaging Conditions: HEK-293cells expressing TRPA1 cannabichromene Rn Agonist 7.2 pEC50 - - 12 ⤷ pEC50 7.2 (EC50 6x10-8 M) [12] Description: Measuring increase in intracellular calcium influx in HEK293 cells expressing rat TRPA1. dibenzoxazepine Hs Activation 7.2 pEC50 - - 26 ⤷ pEC50 7.2 [26] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 loaded with Fluo-4. morphanthridine Hs Activation 7.1 pEC50 - - 26 ⤷ pEC50 7.1 [26] Description: Patch clamp Conditions: HEK293 cells expressing human TRPA1 1'-acetoxychavicol acetate Hs Activation 6.8 pEC50 - - 100 ⤷ pEC50 6.8 [100] Description: FlexStation 2 Calcium imaging Conditions: HEK293 cells expressing human TRPA1 loaded with Fluo-4 chlorobenzylidene malononitrile Hs Activation 6.7 pEC50 - - 26 ⤷ pEC50 6.7 (EC50 1.99x10-7 M) covalent [26] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 loaded with Fluo-4. chloropicrin Hs Activation 6.7 pEC50 - - 19 ⤷ pEC50 6.7 This compound also activates mouse TRPA1 [19] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 and mouse dorsal root ganglion neurons loaded with Fura-2 omega-chloroacetophenone Hs Activation 6.6 pEC50 - - 26 ⤷ pEC50 6.6 [26] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 loaded with Fluo-4. NPPB Hs Activation 6.5 pEC50 - - 82 ⤷ pEC50 6.5 [82] Description: FLIPR calcium influx assay Conditions: HEK293 cells expressing human TRPA1 loaded with Calcium-4 dye benzoquinone Hs Activation 6.4 pEC50 - - 2 ⤷ pEC50 6.4 [2] Description: Calcium imaging Conditions: CHO cells expressing TRPA1 loaded with Fura-2 polygodial Hs Activation 6.4 pEC50 - - 45 ⤷ pEC50 6.4 (EC50 4x10-7 M) [45] cannabidiol Rn Agonist 6.3 pEC50 - - 33 ⤷ pEC50 6.3 (EC50 4.8x10-7 M) [33] isovelleral Hs Activation 6.3 pEC50 - - 45 ⤷ pEC50 6.3 This compound is also an activator of mouse TRPA1. [45] Description: Calcium imaging Conditions: HEK293 cells expressing human or mouse TRPA1 ASP7663 Mm Activation 6.3 pEC50 - - 72 ⤷ pEC50 6.3 (EC50 5x10-7 M) [72] Description: Ligand-induced increase in intracellular Ca2+ in HEK293 cells expressing mTrpa1. ASP7663 Hs Activation 6.3 pEC50 - - 72 ⤷ pEC50 6.3 (EC50 5.1x10-7 M) [72] Description: Ligand-induced increase in intracellular Ca2+ in HEK293 cells expressing hTRPA1. ASP7663 Rn Activation 6.3 pEC50 - - 72 ⤷ pEC50 6.3 (EC50 5.4x10-7 M) [72] Description: Ligand-induced increase in intracellular Ca2+ in HEK293 cells expressing rTrpa1. Cu2+ Mm Activation 6.2 pEC50 - - 4,95 ⤷ pEC50 6.2 (EC50 6x10-7 M) [4,95] cannabigerol Rn Agonist 6.2 pEC50 - - 51 ⤷ pEC50 6.2 (EC50 7x10-7 M) [51] super cinnamaldehyde Mm Activation 6.1 pEC50 - - 85 ⤷ pEC50 6.1 (EC50 8x10-7 M) [85] Description: Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay Conditions: CHO cells expressing mouse TRPA1 bromoacetone Hs Activation 6.0 pEC50 - - 19 ⤷ pEC50 6.0 This compound also activates mouse TRPA1 [19] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 and mouse dorsal root ganglion neurons loaded with Fura-2dorsal root ganglion neurons auranofin Hs Activation 6.0 pEC50 - - 58 ⤷ pEC50 6.0 [58] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 loaded with Fura-2 phytocannabinoid 6 [PMID: 38408345] Rn Agonist 6.0 pEC50 - - 51 ⤷ pEC50 6.0 (EC50 1x10-6 M) [51] allicin Mm Agonist 5.9 pEC50 - Physiological 86 ⤷ pEC50 5.9 [86] Holding voltage: Physiological Cu2+ Hs Activation 5.9 pEC50 - - 4,95 ⤷ pEC50 5.9 (EC50 1.3x10-6 M) [4,95] Description: Sodium imaging Conditions: CHO cells expressing human TRPA1 Cd2+ Hs Activation 5.8 pEC50 - - 4,95 ⤷ pEC50 5.8 (EC50 1.4x10-6 M) [4,95] Description: Sodium and calcium imaging Conditions: CHO cells expressing human TRPA1 and mouse dorsal root ganglion neurons artepillin C Hs Activation 5.7 pEC50 - - 56 ⤷ pEC50 5.7 (EC50 1.8x10-6 M) [56] Description: Calcium imaging Conditions: HEK293 cells transfected with human TRPA1 loaded with Fura-2 4-oxo-nonenal Mm Activation 5.7 pEC50 - - 3 ⤷ pEC50 5.7 [3] Description: Calcium imaging Conditions: CHO cells expressing mouse TRPA1 loaded with Fura-2 nitrooleic acid Hs Activation 5.7 pEC50 - - 138 ⤷ pEC50 5.7 This compound has a similar activity at mouse TRPA1 [138] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 and mouse trigeminal and vagal neurons loaded with Fura-2 Cd2+ Mm Activation 5.7 pEC50 - - 4,95 ⤷ pEC50 5.7 (EC50 2.1x10-6 M) [4,95] 1,6-hexamethylene diisocyanate Hs Activation 5.6 pEC50 - - 19 ⤷ pEC50 5.6 This compound also activates mouse TRPA1 [19] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 and mouse dorsal root ganglion neurons loaded with Fura-2 N-acetyl-4-benzoquinoneimine Rn Activation 5.6 pEC50 - - 2,103 ⤷ pEC50 5.6 This compound has similar activity at human and mouse TRPA1 [2,103] Description: Calcium imaging Conditions: CHO or HEK293 cells expressing rat/mouse/human TRPA1 loaded with Fura-2 oleocanthal Hs Activation 5.6 pEC50 - -60.0 116 ⤷ pEC50 5.6 [116] Holding voltage: -60.0 mV Description: Patch clamp Conditions: HEK-293 cells expressing human TRPA1 O3 Hs Activation 5.5 pEC50 - - 139 ⤷ pEC50 5.5 Ozone has similar activity at mouse TRPA1 [139] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 and mouse vagal neurons loaded with Fura-2 2-pentenal ? Activation 5.3 pEC50 - - 12 ⤷ pEC50 5.3 (EC50 5x10-6 M) [12] acrolein Hs Agonist 5.3 pEC50 - Physiological 14 ⤷ pEC50 5.3 (EC50 5.011x10-6 M) covalent [14] Holding voltage: Physiological salirasib Hs Activation 5.3 pEC50 - - 89 ⤷ pEC50 5.3 [89] Description: FLIPR calcium-influx assay Conditions: CHO-TREx cells loaded with Fluo-3 cannabigeroquinone Rn Agonist 5.1 pEC50 - - 51 ⤷ pEC50 5.1 (EC50 7.8x10-6 M) [51] apomorphine Hs Activation 5.1 pEC50 - - 125 ⤷ pEC50 5.1 Apomorphine blocks TRPA1 at 100µM [125] Description: Calcium imaging, patch clamp Conditions: HEK293 cells transfected with human TRPA1 allicin Hs Agonist 5.1 pEC50 - Physiological 15 ⤷ pEC50 5.1 (EC50 7.943x10-6 M) covalent [15] Holding voltage: Physiological allyl isothiocyanate Rn Activation 5.0 pEC50 - -40.0 64 ⤷ pEC50 5.0 [64] Holding voltage: -40.0 mV cannabidiolic acid Rn Agonist 4.9 pEC50 - - 12 ⤷ pEC50 4.9 (EC50 1.2x10-5 M) [12] Description: Activation of calcium flux via rTrpA1 expressed in HEK293 cells. Δ9-tetrahydrocannabinol Hs Agonist 4.9 pEC50 - -60.0 64 ⤷ pEC50 4.9 (EC50 1.259x10-5 M) non-covalent [64] Holding voltage: -60.0 mV benzyl bromide Hs Activation 4.9 pEC50 - - 19 ⤷ pEC50 4.9 This compound also activates mouse TRPA1 [19] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 and mouse dorsal root ganglion neurons loaded with Fura-2 nicotine Hs Activation 4.8 pEC50 - -75.0 137 ⤷ pEC50 4.8 (EC50 1.7x10-5 M) non-covalent [137] Holding voltage: -75.0 mV Description: Patch clamp Conditions: CHO cells expressing mouse or human TRPA1 allyl isothiocyanate Mm Activation 4.7 pEC50 - Physiological 9 ⤷ pEC50 4.7 [9] Holding voltage: Physiological thymol Hs Activation 4.7 pEC50 6.25x10-6 - 2.5x10-5 - 80 ⤷ pEC50 4.7 (EC50 2x10-5 M) Conc range: 6.25x10-6 - 2.5x10-5 M non-covalent [80] Description: FLIPR calcium influx assay Conditions: Human TRPA1-HEK293 stable cell line loaded with calcium 3 dye URB597 Hs Agonist 4.6 pEC50 - - 108 ⤷ pEC50 4.6 (EC50 2.4x10-5 M) non-covalent [108] Description: Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay Conditions: HEK293 cells expressing human TRPA1 4-hydroxynonenal Rn Activation 4.6 pEC50 - - 88,143 ⤷ pEC50 4.6 [88,143] Description: Calcium imaging Conditions: Rat dorsal root ganglion neurons prostaglandin A2 Mm Activation 4.6 pEC50 - - 90 ⤷ pEC50 4.6 [90] Description: Calcium imaging Conditions: Mouse dorsal root ganglion neurons loaded with Fura-2 crotylaldehyde Rn Activation 4.6 pEC50 - - 6 ⤷ pEC50 4.6 [6] Description: Calcium imaging Conditions: HEK293 cells expressing rat TRPA1 loaded with Fura-2 methyl isocyanate Hs Activation 4.6 pEC50 - - 19 ⤷ pEC50 4.6 This compound also activates mouse TRPA1 [19] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 and mouse dorsal root ganglion neurons loaded with Fura-2 dibutyl phthalate Hs Activation 4.6 pEC50 - - 127 ⤷ pEC50 4.6 [127] Description: Calcium imaging Conditions: CHO cells stably expressing human TRPA1 loaded with Fluo-4 docosahexaenoic acid Rn Activation 4.4 pEC50 - -60.0 96 ⤷ pEC50 4.4 This compound has similar activity at human and mouse TRPA1 [96] Holding voltage: -60.0 mV Description: Patch clamp Conditions: HEK293 celss expressing rat TRPA1 (-)-menthol Hs Partial agonist 4.0 – 4.5 pEC50 - - 65,154 ⤷ pEC50 4.0 – 4.5 (EC50 9.5x10-5 – 2.84x10-5 M) Menthol is also active at the mouse TRPA1, but becomes inhibitory at >100µM [65,154] Description: Calcium imaging, patch clamp Conditions: CHO cells expressing human TRPA1 methylglyoxal Hs Activation 2.5 – 6.0 pEC50 - - 29,40,71 ⤷ pEC50 2.5 – 6.0 This compound has similar activity at mouse and rat TRPA1 [29,40,71] Description: Calcium imaging, patch clamp Conditions: HEK 293 cells expressing hTRPA1, rTRPA1 loaded with Fura-2 allyl isothiocyanate Hs Activation 4.2 pEC50 - - 59 ⤷ pEC50 4.2 (EC50 6.31x10-5 M) [59] cinnamaldehyde Mm Agonist 4.2 pEC50 - Physiological 9 ⤷ pEC50 4.2 (EC50 6.3x10-5 M) covalent [9] Holding voltage: Physiological acetaldehyde Hs Activation 4.1 pEC50 - - 10 ⤷ pEC50 4.1 [10] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 loaded with Fluo-3 flufenamic acid Rn Activation 3.8 pEC50 - -100.0 62 ⤷ pEC50 3.8 [62] Holding voltage: -100.0 mV Description: Two electrode voltage clamp Conditions: Xenopus oocytes expressing rat TRPA1 isoflurane Rn Activation 3.7 pEC50 - - 91 ⤷ pEC50 3.7 [91] Description: Patch clamp Conditions: HEK293 cells expressing rat TRPA1 H2O2 Mm Activation 3.6 pEC50 - - 3,123 ⤷ pEC50 3.6 [3,123] Description: Calcium imaging Conditions: CHO cells expressing mouse TRPA1 loaded with Fura-2 2-iodoacetamide Mm Activation 3.5 pEC50 - - 85 ⤷ pEC50 3.5 (EC50 3.57x10-4 M) [85] Description: Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay Conditions: CHO cells expressing mouse TRPA1 formalin Mm Activation 3.4 pEC50 - - 88,92 ⤷ pEC50 3.4 (EC50 3.981x10-4 M) covalent. This level of activity is also observed for rat TRPA1 [88,92] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 loaded with Fluo-4 niflumic acid Rn Activation 3.3 pEC50 - -100.0 62 ⤷ pEC50 3.3 [62] Holding voltage: -100.0 mV Description: Two electrode voltage clamp Conditions: Xenopus oocytes expressing rat TRPA1 acetaldehyde Mm Activation 2.9 pEC50 - - 10 ⤷ pEC50 2.9 [10] Description: Calcium imaging Conditions: HEK293 cells expressing mouse TRPA1loaded with Fluo-3 NaHS Mm Activation 2.9 pEC50 - - 133 ⤷ pEC50 2.9 This compound has similar activity at the human TRPA1 [133] Description: Calcium imaging Conditions: HEK293 cells expressing mouse TRPA1 loaded with Fura-2 MTSEA Mm Activation 2.8 pEC50 - - 85 ⤷ pEC50 2.8 (EC50 1.58x10-3 M) [85] Description: Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay Conditions: CHO cells expressing mouse TRPA1 methyl p-hydroxybenzoate Mm Activation 2.4 pEC50 - -60.0 49 ⤷ pEC50 2.4 [49] Holding voltage: -60.0 mV Description: Patch clamp Conditions: HEK293 cells expressing mouse TRPA1 Zn2+ Mm Activation 2.3 pEC50 - - 4,61 ⤷ pEC50 2.3 Zinc has similar activity at the human TRPA1 [4,61] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 and mouse dorsal root ganglia neurons loaded with Fura-2 NH4Cl Mm Activation 2.0 pEC50 - - 50 ⤷ pEC50 2.0 [50] Description: Patch clamp Conditions: HEK293 cells expressing mouse TRPA1 PF-4840154 Rn Activation 7.0 pIC50 - - 122 ⤷ pIC50 7.0 (IC50 1x10-7 M) [122]
View species-specific activator tables
Activator Comments
TRPA1 is activated by covalent modification of intracellular cysteines [59], activated by bradykinin [9,14,64], probably activated by noxious cold [9,131], but this is disputed [64,98], mechano-activation is still under discussion. TRPA1 is modulated by intra- and extracellular Ca2+ [98]. Snake and fly TRPA1 are a heat-activated channels [52,107,148]. In a calcium imaging study the PGD2 metabolite 15-deoxy-Δ12,14-prostaglandin J2 activated the human TRPA1 expressed in HEK293 cells and in a subset of chemosensitive mouse trigeminal neurons, where this activation was blocked by both the nonselective TRP channel blocker ruthenium red, and the TRPA1 inhibitor HC-030031. Δ12-PGJ2 and 8-iso-PGA2 are also activators of TRPA1 [140]. Further compounds which are reported to activate TRPA1 in vitro include: 2-pentenal (mouse) [14], clotrimazole (human and mouse) [94], WIN55212-2 (mouse) [1] and AM1241 (mouse) [1], sodium hypochlorite (NaOCl; mouse and human) [20], 5,6-EET (mouse) [128], hepoxilin A3 (mouse, rat) [54], 12S-HPETE (mouse, rat) [54], carbon dioxide (rat, mouse) [150], acetic, propinoic, formic, and lactic acids (human, rat, mouse) [149].

Inhibitors
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Ligand Sp. Action Value Parameter Concentration range (M) Holding voltage (mV) Reference AM-0902 Rn Antagonist 7.6 pIC50 - - 124 ⤷ pIC50 7.6 (IC50 2.4x10-8 M) [124] Description: Antagonism of activator-induced calcium flux measuring 45Ca2+.

Gating inhibitors
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Ligand Sp. Action Value Parameter Concentration range (M) Holding voltage (mV) Reference resolvin D2 Mm Inhibition 8.7 pIC50 - -60.0 112 ⤷ pIC50 8.7 [112] Holding voltage: -60.0 mV Description: Patch-clamp Conditions: Mouse DRG neurons, mustard oil AITC (300 µM) resolvin D1 Mm Inhibition 7.2 pIC50 - - 11,112 ⤷ pIC50 7.2 [11,112] Description: Calcium imaging, patch clamp Conditions: Mouse DRG neurons, mustard oil AITC (300 µM); HEK293T cells transfected with mTRPs AP18 Hs Inhibition 5.5 pIC50 - - 115 ⤷ pIC50 5.5 (IC50 3.1x10-6 M) [115] Description: Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay Conditions: CHO cells expressing human TRPA1 AP18 Mm Inhibition 5.3 pIC50 - - 115 ⤷ pIC50 5.3 (IC50 4.5x10-6 M) [115] Description: Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay gentamicin Mm Antagonist 5.2 pIC50 - -80.0 98 ⤷ pIC50 5.2 [98] Holding voltage: -80.0 mV HC030031 Hs Inhibition 5.2 pIC50 - - 92 ⤷ pIC50 5.2 [92] Description: Calcium imaging Conditions: HEK293 cells expressing human TRPA1 loaded with Fluo-4 isopentenyl diphosphate Mm Inhibition 5.1 pIC50 - - 11 ⤷ pIC50 5.1 [11] Description: Calcium imaging Conditions: HEK-293 cells expressing TRPA1 TCS 5861528 Hs Inhibition 4.8 pIC50 - - 151 ⤷ pIC50 4.8 [151] Description: Calcium imaging Conditions: Human TRPA1-inducible HEK-293 cells (HEK-LacltrpA1 clone B22), Aallyl isothiocyanate as agonist camphor Mm Antagonist 4.2 pIC50 - Physiological 87 ⤷ pIC50 4.2 [87] Holding voltage: Physiological (-)-menthol Mm Antagonist 4.2 pIC50 - Physiological 87 ⤷ pIC50 4.2 [87] Holding voltage: Physiological
View species-specific gating inhibitor tables

Antagonists
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Ligand Sp. Action Value Parameter Reference GDC-6599 Hs Inhibition 8.0 pIC50 141 ⤷ pIC50 8.0 (IC50 9.38x10-9 M) [141]

Channel Blockers
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Ligand Sp. Action Value Parameter Concentration range (M) Holding voltage (mV) Reference GDC-0334 Hs Inhibition 8.8 pIC50 - - 8 ⤷ pIC50 8.8 (IC50 1.69x10-9 M) [8] AM-0902 Hs Antagonist 7.7 pIC50 - - 124 ⤷ pIC50 7.7 (IC50 2x10-8 M) [124] Description: Antagonism of activator-induced calcium flux measuring 45Ca2+. A-967079 Hs Inhibition 7.2 pIC50 - - 32 ⤷ pIC50 7.2 This compoud also acts as a gating inhibitor at the rat and mouse TRPA1. [32] Description: Calcium imaging Conditions: HEK-293F cells expressing TRPA1 Gd3+ Mm Antagonist 7.0 pIC50 - -80.0 98 ⤷ pIC50 7.0 [98] Holding voltage: -80.0 mV ruthenium red Mm Inhibition 5.5 pIC50 - -80.0 98 ⤷ pIC50 5.5 (IC50 3.55x10-6 M) [98] Holding voltage: -80.0 mV amiloride Mm Inhibition 3.3 pIC50 - -80.0 98 ⤷ pIC50 3.3 [98] Holding voltage: -80.0 mV
View species-specific channel blocker tables
Channel Blocker Comments
Blocking effects are modulated by divalent cations [98].

Immunopharmacology Comments

Several lines of evidence implicate TRPA1 in inflammation, inflammatory pain and inflammatory diseases [76,84,93,114,132,156].

Cell Type Associations

Immuno Cell Type:  Mast cells Comment:  TRPA1 is reported to be involved mast cell secretory granule formation in rat. References:  111

Tissue Distribution
Brain, heart, small intestine, lung, skeletal muscle, and pancreas. Species:  Human Technique:  Northern Blot References:  130
Gastrointestinal tissues (including stomach, intestine, epithelial cell, duodenal mucosa), enterochromaffin cells. NOTE: this pattern of expression is also reported in mouse. Species:  Human Technique:  RT-PCR, in situ hybridization, flow cytometoric analysis References:  73,109,