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company name :
Tocris Bioscience
product type :
chemical
product name :
0464/10
catalog :
0464/10
quantity :
10 mg (also 50 mg)
price :
230 USD
more info or order :
citations: 57
Reference
Cheng R, Feng Y, Liu D, Wang Z, Zhang J, Chen L, et al. The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes. Theranostics. 2019;9:4287-4307 pubmed publisher
Diniz C, Biojone C, Joca S, Rantamäki T, Castren E, Guimarães F, et al. Dual mechanism of TRKB activation by anandamide through CB1 and TRPV1 receptors. Peerj. 2019;7:e6493 pubmed publisher
Kamiya K, Osaki T, Nakao K, Kawano R, Fujii S, Misawa N, et al. Electrophysiological measurement of ion channels on plasma/organelle membranes using an on-chip lipid bilayer system. Sci Rep. 2018;8:17498 pubmed publisher
Balleza Tapia H, Crux S, Andrade Talavera Y, Dolz Gaiton P, Papadia D, Chen G, et al. TrpV1 receptor activation rescues neuronal function and network gamma oscillations from Aβ-induced impairment in mouse hippocampus in vitro. elife. 2018;7: pubmed publisher
Saliba S, Marcotegui A, Fortwängler E, Ditrich J, Perazzo J, Munoz E, et al. AM404, paracetamol metabolite, prevents prostaglandin synthesis in activated microglia by inhibiting COX activity. J Neuroinflammation. 2017;14:246 pubmed publisher
Wu N, Tasker J. Nongenomic Glucocorticoid Suppression of a Postsynaptic Potassium Current via Emergent Autocrine Endocannabinoid Signaling in Hypothalamic Neuroendocrine Cells following Chronic Dehydration. Eneuro. 2017;4: pubmed publisher
Hofmann M, Andresen M. Dynasore blocks evoked release while augmenting spontaneous synaptic transmission from primary visceral afferents. PLoS ONE. 2017;12:e0174915 pubmed publisher
Wang X, Tian B, Huang Y, Peng X, Chen L, Li J, et al. Hydrogen sulfide-induced itch requires activation of Cav3.2 T-type calcium channel in mice. Sci Rep. 2015;5:16768 pubmed publisher
Vijayvergiya V, Acharya S, Wilson S, Schmidt J. Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers. PLoS ONE. 2015;10:e0141366 pubmed publisher
Smith M, Wilson R, O Brien S, Tufarelli C, Anderson S, O Sullivan S. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation. PLoS ONE. 2015;10:e0136546 pubmed publisher
Eskander M, Ruparel S, Green D, Chen P, Por E, Jeske N, et al. Persistent Nociception Triggered by Nerve Growth Factor (NGF) Is Mediated by TRPV1 and Oxidative Mechanisms. J Neurosci. 2015;35:8593-603 pubmed publisher
Ma X, Zhang F, Dong F, Bao L, Zhang X. Experimental evidence for alleviating nociceptive hypersensitivity by single application of capsaicin. Mol Pain. 2015;11:22 pubmed publisher
Lin T, Lu C, Wu C, Huang S, Wang S. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. Int J Mol Sci. 2015;16:5555-71 pubmed publisher
Rossi S, Motta C, Studer V, Macchiarulo G, Volpe E, Barbieri F, et al. Interleukin-1β causes excitotoxic neurodegeneration and multiple sclerosis disease progression by activating the apoptotic protein p53. Mol Neurodegener. 2014;9:56 pubmed publisher
Morelli M, Amantini C, Nabissi M, Liberati S, Cardinali C, Farfariello V, et al. Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation. BMC Cancer. 2014;14:921 pubmed publisher
Borrelli F, Romano B, Petrosino S, Pagano E, Capasso R, Coppola D, et al. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent. Br J Pharmacol. 2015;172:142-58 pubmed publisher
Wang G, Wang X, Liu S, Qu M, Xia Y, Needleman B, et al. Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine. Am J Physiol Gastrointest Liver Physiol. 2014;307:G719-31 pubmed publisher
Nguyen T, Kwon S, Hong S, Ma S, Jung Y, Hwang J, et al. Transient receptor potential vanilloid type 1 channel may modulate opioid reward. Neuropsychopharmacology. 2014;39:2414-22 pubmed publisher
Lu W, Li J, Gong L, Xu X, Han T, Ye Y, et al. H2 S modulates duodenal motility in male rats via activating TRPV1 and K(ATP) channels. Br J Pharmacol. 2014;171:1534-50 pubmed publisher
Maleńczyk K, Jazurek M, Keimpema E, Silvestri C, Janikiewicz J, Mackie K, et al. CB1 cannabinoid receptors couple to focal adhesion kinase to control insulin release. J Biol Chem. 2013;288:32685-99 pubmed publisher
Graham D, Huang L, Robinson K, Messerli M. Epidermal keratinocyte polarity and motility require Ca²? influx through TRPV1. J Cell Sci. 2013;126:4602-13 pubmed publisher
Derbenev A, Smith B. Dexamethasone rapidly increases GABA release in the dorsal motor nucleus of the vagus via retrograde messenger-mediated enhancement of TRPV1 activity. PLoS ONE. 2013;8:e70505 pubmed publisher
Ruparel S, Green D, Chen P, Hargreaves K. The cytochrome P450 inhibitor, ketoconazole, inhibits oxidized linoleic acid metabolite-mediated peripheral inflammatory pain. Mol Pain. 2012;8:73 pubmed publisher
Liu X, Jutooru I, Lei P, Kim K, Lee S, Brents L, et al. Betulinic acid targets YY1 and ErbB2 through cannabinoid receptor-dependent disruption of microRNA-27a:ZBTB10 in breast cancer. Mol Cancer Ther. 2012;11:1421-31 pubmed publisher
Albert E, Bec J, Desmadryl G, Chekroud K, Travo C, Gaboyard S, et al. TRPV4 channels mediate the infrared laser-evoked response in sensory neurons. J Neurophysiol. 2012;107:3227-34 pubmed publisher
Muzzi M, Felici R, Cavone L, Gerace E, Minassi A, Appendino G, et al. Ischemic neuroprotection by TRPV1 receptor-induced hypothermia. J Cereb Blood Flow Metab. 2012;32:978-82 pubmed publisher
Fox J, Sakamuru S, Huang R, Teneva N, Simmons S, Xia M, et al. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death. Proc Natl Acad Sci U S A. 2012;109:5423-8 pubmed publisher
Hamtiaux L, Masquelier J, Muccioli G, Bouzin C, Feron O, Gallez B, et al. The association of N-palmitoylethanolamine with the FAAH inhibitor URB597 impairs melanoma growth through a supra-additive action. BMC Cancer. 2012;12:92 pubmed publisher
Hamtiaux L, Hansoulle L, Dauguet N, Muccioli G, Gallez B, Lambert D. Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism. PLoS ONE. 2011;6:e26823 pubmed publisher
Kaszas K, Keller J, Coddou C, Mishra S, Hoon M, Stojilkovic S, et al. Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH. J Pharmacol Exp Ther. 2012;340:152-60 pubmed publisher
Canetta S, Luca E, Pertot E, Role L, Talmage D. Type III Nrg1 back signaling enhances functional TRPV1 along sensory axons contributing to basal and inflammatory thermal pain sensation. PLoS ONE. 2011;6:e25108 pubmed publisher
Casarotto P, Terzian A, Aguiar D, Zangrossi H, Guimarães F, Wotjak C, et al. Opposing roles for cannabinoid receptor type-1 (CB?) and transient receptor potential vanilloid type-1 channel (TRPV1) on the modulation of panic-like responses in rats. Neuropsychopharmacology. 2012;37:478-86 pubmed publisher
Li Q, Burrell B. Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms. Learn Mem. 2011;18:545-53 pubmed publisher
Ruparel N, Patwardhan A, Akopian A, Hargreaves K. Desensitization of transient receptor potential ankyrin 1 (TRPA1) by the TRP vanilloid 1-selective cannabinoid arachidonoyl-2 chloroethanolamine. Mol Pharmacol. 2011;80:117-23 pubmed publisher
Samineni V, Premkumar L, Faingold C. Post-ictal analgesia in genetically epilepsy-prone rats is induced by audiogenic seizures and involves cannabinoid receptors in the periaqueductal gray. Brain Res. 2011;1389:177-82 pubmed publisher
Yuan S, Burrell B. Endocannabinoid-dependent LTD in a nociceptive synapse requires activation of a presynaptic TRPV-like receptor. J Neurophysiol. 2010;104:2766-77 pubmed publisher
Kim J, Alger B. Reduction in endocannabinoid tone is a homeostatic mechanism for specific inhibitory synapses. Nat Neurosci. 2010;13:592-600 pubmed publisher
Bhaskaran M, Smith B. Effects of TRPV1 activation on synaptic excitation in the dentate gyrus of a mouse model of temporal lobe epilepsy. Exp Neurol. 2010;223:529-36 pubmed publisher
Buznikov G, Nikitina L, Bezuglov V, Francisco M, Boysen G, Obispo Peak I, et al. A putative 'pre-nervous' endocannabinoid system in early echinoderm development. Dev Neurosci. 2010;32:1-18 pubmed publisher
Melis M, Pillolla G, Luchicchi A, Muntoni A, Yasar S, Goldberg S, et al. Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic dopamine neurons through nuclear receptors. J Neurosci. 2008;28:13985-94 pubmed publisher
Gibson H, Edwards J, Page R, Van Hook M, Kauer J. TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons. Neuron. 2008;57:746-59 pubmed publisher
Bambico F, Katz N, Debonnel G, Gobbi G. Cannabinoids elicit antidepressant-like behavior and activate serotonergic neurons through the medial prefrontal cortex. J Neurosci. 2007;27:11700-11 pubmed
Benninger F, Freund T, Hajos N. Control of excitatory synaptic transmission by capsaicin is unaltered in TRPV1 vanilloid receptor knockout mice. Neurochem Int. 2008;52:89-94 pubmed
Moezi L, Gaskari S, Liu H, Baik S, Dehpour A, Lee S. Anandamide mediates hyperdynamic circulation in cirrhotic rats via CB(1) and VR(1) receptors. Br J Pharmacol. 2006;149:898-908 pubmed
Akerman S, Holland P, Goadsby P. Cannabinoid (CB1) receptor activation inhibits trigeminovascular neurons. J Pharmacol Exp Ther. 2007;320:64-71 pubmed
Bautista D, Movahed P, Hinman A, Axelsson H, Sterner O, Hogestatt E, et al. Pungent products from garlic activate the sensory ion channel TRPA1. Proc Natl Acad Sci U S A. 2005;102:12248-52 pubmed
Kwolek G, Zakrzeska A, Schlicker E, Gothert M, Godlewski G, Malinowska B. Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats. Br J Pharmacol. 2005;145:567-75 pubmed
Gavva N, Tamir R, Qu Y, Klionsky L, Zhang T, Immke D, et al. AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties. J Pharmacol Exp Ther. 2005;313:474-84 pubmed
Baker C, McDougall J. The cannabinomimetic arachidonyl-2-chloroethylamide (ACEA) acts on capsaicin-sensitive TRPV1 receptors but not cannabinoid receptors in rat joints. Br J Pharmacol. 2004;142:1361-7 pubmed
Akerman S, Kaube H, Goadsby P. Anandamide acts as a vasodilator of dural blood vessels in vivo by activating TRPV1 receptors. Br J Pharmacol. 2004;142:1354-60 pubmed
Price T, Patwardhan A, Akopian A, Hargreaves K, Flores C. Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons. Br J Pharmacol. 2004;142:257-66 pubmed
Melis M, Pistis M, Perra S, Muntoni A, Pillolla G, Gessa G. Endocannabinoids mediate presynaptic inhibition of glutamatergic transmission in rat ventral tegmental area dopamine neurons through activation of CB1 receptors. J Neurosci. 2004;24:53-62 pubmed
Akerman S, Kaube H, Goadsby P. Vanilloid type 1 receptors (VR1) on trigeminal sensory nerve fibres play a minor role in neurogenic dural vasodilatation, and are involved in capsaicin-induced dural dilation. Br J Pharmacol. 2003;140:718-24 pubmed
Kagaya M, Lamb J, Robbins J, Page C, Spina D. Characterization of the anandamide induced depolarization of guinea-pig isolated vagus nerve. Br J Pharmacol. 2002;137:39-48 pubmed
Mazzone S, Canning B. Synergistic interactions between airway afferent nerve subtypes mediating reflex bronchospasm in guinea pigs. Am J Physiol Regul Integr Comp Physiol. 2002;283:R86-98 pubmed
Craib S, Ellington H, Pertwee R, Ross R. A possible role of lipoxygenase in the activation of vanilloid receptors by anandamide in the guinea-pig bronchus. Br J Pharmacol. 2001;134:30-7 pubmed
Izzo A, Capasso R, Pinto L, Di Carlo G, Mascolo N, Capasso F. Effect of vanilloid drugs on gastrointestinal transit in mice. Br J Pharmacol. 2001;132:1411-6 pubmed
image
image 1 :
Tocris Bioscience 0464/10 image 1
Cat.No. 0464 - Capsazepine C19H21ClN2O2S CAS No. 138977-28-3
product information
master code :
464
SKU :
0464/10
product name :
Capsazepine
unit size :
10 mg (also 50 mg)
description :
TRPV antagonist; also activator of ENaC
target :
TRPV Antagonists
category :
Small Molecules
purity :
99%
observed molecular weight :
376.9
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
Capsazepine is a selective vanilloid receptor antagonist (Ki = 3.2 u M). Inhibits carrageenan inflammation-induced hyperalgesic responses in the rat. Also activates amiloride-sensitive epithelial Na+ channel ENaC .
top caption :
TRPV antagonist; also activator of ENaC
extended description :
TRPV antagonist; also activator of ENaC
chemical name text :
N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide
formula :
C19H21ClN2O2S
formula text :
C19H21ClN2O2S
cas num :
138977-28-3
USD :
230 USD
product details :
TRPV antagonist; also activator of ENaC
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK