Capsazepine

Cat. No. 0464

Capsazepine C19H21ClN2O2S [138977-28-3]

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Chemical Name: N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide

Biological Activity

Selective vanilloid receptor antagonist (Ki = 3.2 μM). Inhibits carrageenan inflammation-induced hyperalgesic responses in the rat. Also activates amiloride-sensitive epithelial Na+ channel ENaCδ. Also available as part of the Vanilloid TRPV1 Receptor Tocriset™.

Technical Data

M.Wt:
376.9
Formula:
C19H21ClN2O2S
Solubility:
Soluble to 25 mM in ethanol and to 100 mM in DMSO
Purity:
>99 %
Storage:
Store at RT
CAS No:
138977-28-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Yamamura et al (2004) Capsazepine is a novel activator of the δ subunit of the human epithelial Na+ channel. J.Biol.Chem. 279 44483. PMID: 15308635.

Kwak et al (1998) A capsaicin-receptor antagonist, capsazepine, reduces inflammation-induced hyperalgesic responses in the rat: evidence for an endogenous capsaicin-like substance. Neuroscience 86 619. PMID: 9881874.

Dickenson and Dray (1991) Selective antagonism of capsaicin by capsazepine: evidence for a spinal receptor site in capsaicin-induced antinociception. Br.J.Pharmacol. 104 1045. PMID: 1810591.

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Citations are publications that use Tocris products. Selected citations for Capsazepine include:

Ma et al (2015) Experimental evidence for alleviating nociceptive hypersensitivity by single application of capsaicin. Mol Pain 11 22. PMID: 25896608.

Morelli et al (2014) Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation. BMC Cancer 14 921. PMID: 25481381.

Nguyen et al (2014) Transient receptor potential vanilloid type 1 channel may modulate opioid reward. Neuropsychopharmacology 39 2414. PMID: 24732880.

Rossi et al (2014) Interleukin-1β causes excitotoxic neurodegeneration and multiple sclerosis disease progression by activating the apoptotic protein p53. Mol Neurodegener 9 56. PMID: 25495224.

Wang et al (2014) Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine. Am J Physiol Gastrointest Liver Physiol 307 G719. PMID: 25147231.

Graham et al (2013) Epidermal keratinocyte polarity and motility require Ca2+ influx through TRPV1. J Cell Sci 126 4602. PMID: 23943873.

Malenczyk et al (2013) CB1 cannabinoid receptors couple to focal adhesion kinase to control insulin release. J Biol Chem 288 32685. PMID: 24089517.

Albert et al (2012) TRPV4 channels mediate the infrared laser-evoked response in sensory neurons. J Neurophysiol 107 3227. PMID: 22442563.

Liu et al (2012) Betulinic acid targets YY1 and ErbB2 through cannabinoid receptor-dependent disruption of microRNA-27a:ZBTB10 in breast cancer. Mol Cancer Ther 11 1421. PMID: 22553354.

Li and Burrell (2011) Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms. Learn Mem 18 545. PMID: 21844187.

Kim and Alger (2010) Reduction in endocannabinoid tone is a homeostatic mechanism for specific inhibitory synapses. Nat Neurosci 13 592. PMID: 20348918.

Yuan and Burrell (2010) Endocannabinoid-dependent LTD in a nociceptive synapse requires activation of a presynaptic TRPV-like receptor. J Neurophysiol 104 2766. PMID: 20884761.

Gibson et al (2008) TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons. Neuron 57 746. PMID: 18341994.

Melis et al (2008) Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic dopamine neurons through nuclear receptors. J Neurosci 28 13985. PMID: 19091987.

Gavva et al (2005) 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 313 474. PMID: 15615864.

Kwolek et al (2005) Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats. Br J Pharmacol 145 567. PMID: 15834445.

Akerman et al (2004) Anandamide acts as a vasodilator of dural blood vessels in vivo by activating TRPV1 receptors. Br J Pharmacol 142 1354. PMID: 15277315.

Price et al (2004) Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons. Br J Pharmacol 142 257. PMID: 15155534.

Do you know of a great paper that uses Capsazepine from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: Capsazepine, supplier, Vanilloid, receptor, antagonists, activators, ENaCdelta, vanilloid, Vanillioid, Receptors, VR1, TRPV, TRP, Channels, Transient, Receptor, Potential, Sodium, Epithelial, ENaC, Na+, Tocris Bioscience, TRPV Antagonist products

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