Chemical Name: 2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(4-isopropylphenyl)acetamide
Biological ActivityHC 030031 is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx (IC50 values are 6.2 and 5.3 μM respectively). Does not block currents mediated by TRPV1, TRPV3, TRPV4, hERG or NaV1.2 channels. Inhibits AITC- and formalin-induced flinching in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Prostaglandin-induced activation of nociceptive neurons via direct interactions with TRPA1.
Taylor-Clark et al.
TRPA1 mediates formalin-induced pain.
McNamara et al.
Citations for HC 030031
The citations listed below are publications that use Tocris products. Selected citations for HC 030031 include:
31 Citations: Showing 1 - 10
The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes.
Authors: Cheng Et al.
A critical evaluation of TRPA1-mediated locomotor behavior in zebrafish as a screening tool for novel anti-nociceptive drug discovery.
Authors: Ko Et al.
Sci Rep 2019;9:2430
Bladder Dysfunction in an Obese Zucker Rat: The Role of TRPA1 Channels, Oxidative Stress, and Hydrogen Sulfide.
Authors: Blaha Et al.
Oxid Med Cell Longev 2019;2019:5641645
Relevance of TRPA1 and TRPM8 channels as vascular sensors of cold in the cutaneous microvasculature.
Authors: Pan Et al.
Pflugers Arch 2018;470:779
Transient Opening of the Mitochondrial Permeability Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes.
Authors: Agarwal Et al.
TRPA1-FGFR2 binding event is a regulatory oncogenic driver modulated by miRNA-142-3p.
Authors: Berrout Et al.
Nat Commun 2017;8:947
Methylglyoxal Requires AC1 and TRPA1 to Produce Pain and Spinal Neuron Activation.
Authors: Griggs Et al.
Front Neurosci 2017;11:679
Modulation of breast cancer cell viability by a cannabinoid receptor 2 agonist, JWH-015, is calcium dependent.
Authors: Hanlon Et al.
Breast Cancer (Dove Med Press) 2016;8:59
Effects of ε-viniferin, a dehydrodimer of resveratrol, on transepithelial active ion transport and ion permeability in the rat small and large intestinal mucosa.
Authors: Karaki Et al.
Physiol Rep 2016;4
Environmental cold exposure increases blood flow and affects pain sensitivity in the knee joints of CFA-induced arthritic mice in a TRPA1-dependent manner.
Authors: Fernandes Et al.
Mol Pain 2016;18:7
Hydrogen sulfide-induced itch requires activation of Cav3.2 T-type calcium channel in mice.
Authors: Wang Et al.
World J Gastroenterol 2015;5:16768
Structure of the TRPA1 ion channel suggests regulatory mechanisms.
Authors: Paulsen Et al.
Alterations in serotonin, transient receptor potential channels and protease-activated receptors in rats with irritable bowel syndrome attenuated by Shugan decoction.
Authors: Shi Et al.
Arthritis Res Ther 2015;21:4852
Antinociceptive activity of transient receptor potential channel TRPV1, TRPA1, and TRPM8 antagonists in neurogenic and neuropathic pain models in mice.
Authors: Sałat and Filipek
J Neurosci 2015;16:167
Released lipids regulate transient receptor potential channel (TRP)-dependent oral cancer pain.
Authors: Ruparel Et al.
Nat Commun 2015;11:30
Menthol suppresses laryngeal C-fiber hypersensitivity to cigarette smoke in a rat model of gastroesophageal reflux disease: the role of TRPM8.
Authors: Liu Et al.
J Appl Physiol (1985) 2015;118:635
Differential Contribution of TRPA1, TRPV4 and TRPM8 to Colonic Nociception in Mice.
Authors: Mueller-Tribbensee Et al.
PLoS One 2015;10:e0128242
TRPA1 is essential for the vascular response to environmental cold exposure.
Authors: Aubdool Et al.
J Zhejiang Univ Sci B 2014;5:5732
Investigating the potential role of TRPA1 in locomotion and cardiovascular control during hypertension.
Authors: Bodkin Et al.
Pharmacol Res Perspect 2014;2:e00052
Sensory nerve terminal mitochondrial dysfunction activates airway sensory nerves via transient receptor potential (TRP) channels.
Authors: Nesuashvili Et al.
Mol Pharmacol 2013;83:1007
Hydrogen sulfide induces hypersensitivity of rat capsaicin-sensitive lung vagal neurons: role of TRPA1 receptors.
Authors: Hsu Et al.
Am J Physiol Regul Integr Comp Physiol 2013;305:R769
The molecular basis for species-specific activation of human TRPA1 protein by protons involves poorly conserved residues within transmembrane domains 5 and 6.
Authors: Roche Et al.
J Biol Chem 2013;288:20280
Activation of TRPA1 by luminal stimuli induces EP4-mediated anion secretion in human and rat colon.
Authors: Kaji Et al.
Am J Physiol Gastrointest Liver Physiol 2012;302:G690
Oxidative stress induces itch via activation of transient receptor potential subtype ankyrin 1 in mice.
Authors: Liu and Ji
Neurosci Bull 2012;28:145
Involvement of the endogenous hydrogen sulfide/Ca(v) 3.2 T-type Ca2+ channel pathway in cystitis-related bladder pain in mice.
Authors: Matsunami Et al.
Br J Pharmacol 2012;167:917
Inhibitory effect of cannabichromene, a major non-psychotropic cannabinoid extracted from Cannabis sativa, on inflammation-induced hypermotility in mice.
Authors: Izzo Et al.
Br J Pharmacol 2012;166:1444
Modulation of mouse gastrointestinal motility by allyl isothiocyanate, a constituent of cruciferous vegetables (Brassicaceae): evidence for TRPA1-independent effects.
Authors: Capasso Et al.
Br J Pharmacol 2012;165:1966
Spinal 12-lipoxygenase-derived hepoxilin A3 contributes to inflammatory hyperalgesia via activation of TRPV1 and TRPA1 receptors.
Authors: Gregus Et al.
Proc Natl Acad Sci U S A 2012;109:6721
Ocular dryness excites two classes of corneal afferent neurons implicated in basal tearing in rats: involvement of transient receptor potential channels.
J Neurophysiol 2012;107:1199
Effects of luminal thymol on epithelial transport in human and rat colon.
Authors: Kaji Et al.
Am J Physiol Gastrointest Liver Physiol 2011;300:G1132
TRPA1 receptors mediate environmental irritant-induced meningeal vasodilatation.
Authors: Kunkler Et al.
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Reviews for HC 030031
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We used all these compounds which were dissolved in DMSO and added to fresh culture media. Concentration reference paper PMID: 27186076
microinjection of the TRPA1 inhibitor HC 030031 into Drosophila melanogaster embryos. Drug appears to phenocopy aspects of the null mutant and RNAi knockdown of the TRPA1 gene in embryos fairly well.