Capsazepine (CAS 138977-28-3): R&D Systems
Catalog Number: 0464
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.
Background References
  1. Selective antagonism of capsaicin by capsazepine: evidence for a spinal receptor site in capsaicin-induced antinociception.
    Dickenson and Dray
    Br.J.Pharmacol., 1991;104:1045
  2. A capsaicin-receptor antagonist, capsazepine, reduces inflammation-induced hyperalgesic responses in the rat: evidence for an endogenous capsaicin-like substance.
    Kwak et al.
    Neuroscience, 1998;86:619
  3. Capsazepine is a novel activator of the δ subunit of the human epithelial Na+ channel.
    Yamamura et al.
    J.Biol.Chem., 2004;279:44483
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Capsazepine include:

37 Citations: Showing 1 - 10
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  1. Hydrogen sulfide-induced itch requires activation of Cav3.2 T-type calcium channel in mice.
    Authors: Wang Et al.
    Int J Mol Sci 2015;5:16768
  2. Persistent Nociception Triggered by Nerve Growth Factor (NGF) Is Mediated by TRPV1 and Oxidative Mechanisms.
    Authors: Eskander Et al.
    Br J Pharmacol 2015;35:8593
  3. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent.
    Authors: Borrelli Et al.
    PLoS One 2015;172:142
  4. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    J Neurosci 2015;16:5555
  5. Experimental evidence for alleviating nociceptive hypersensitivity by single application of capsaicin.
    Authors: Ma Et al.
    Mol Pain 2015;11:22
  6. Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers.
    Authors: Vijayvergiya Et al.
    PLoS One 2015;10:e0141366
  7. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
    Authors: Smith Et al.
    PLoS One 2015;10:e0136546
  8. Interleukin-1β causes excitotoxic neurodegeneration and multiple sclerosis disease progression by activating the apoptotic protein p53.
    Authors: Rossi Et al.
    Mol Neurodegener 2014;9:56
  9. Transient receptor potential vanilloid type 1 channel may modulate opioid reward.
    Authors: Nguyen Et al.
    Neuropsychopharmacology 2014;39:2414
  10. Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine.
    Authors: Wang Et al.
    Am J Physiol Gastrointest Liver Physiol 2014;307:G719
  11. H2 S modulates duodenal motility in male rats via activating TRPV1 and K(ATP) channels.
    Authors: Lu Et al.
    Proc Natl Acad Sci U S A 2014;171:1534
  12. Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation.
    Authors: Morelli Et al.
    BMC Cancer 2014;14:921
  13. CB1 cannabinoid receptors couple to focal adhesion kinase to control insulin release.
    Authors: Malenczyk Et al.
    J Biol Chem 2013;288:32685
  14. Epidermal keratinocyte polarity and motility require Ca2+ influx through TRPV1.
    Authors: Graham Et al.
    J Cell Sci 2013;126:4602
  15. Opposing roles for cannabinoid receptor type-1 (CB1) and transient receptor potential vanilloid type-1 channel (TRPV1) on the modulation of panic-like responses in rats.
    Authors: Casarotto Et al.
    Br J Pharmacol 2012;37:478
  16. Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH.
    Authors: Kaszás Et al.
    Dev Neurosci 2012;340:152
  17. Ischemic neuroprotection by TRPV1 receptor-induced hypothermia.
    Authors: Muzzi Et al.
    Br J Pharmacol 2012;32:978
  18. Betulinic acid targets YY1 and ErbB2 through cannabinoid receptor-dependent disruption of microRNA-27a:ZBTB10 in breast cancer.
    Authors: Liu Et al.
    Mol Cancer Ther 2012;11:1421
  19. TRPV4 channels mediate the infrared laser-evoked response in sensory neurons.
    Authors: Albert Et al.
    J Neurophysiol 2012;107:3227
  20. Desensitization of transient receptor potential ankyrin 1 (TRPA1) by the TRP vanilloid 1-selective cannabinoid arachidonoyl-2 chloroethanolamine.
    Authors: Ruparel Et al.
    Neurochem Int 2011;80:117
  21. Type III Nrg1 back signaling enhances functional TRPV1 along sensory axons contributing to basal and inflammatory thermal pain sensation.
    Authors: Canetta Et al.
    J Cereb Blood Flow Metab 2011;6:e25108
  22. Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms.
    Authors: Li and Burrell
    Learn Mem 2011;18:545
  23. A putative 'pre-nervous' endocannabinoid system in early echinoderm development.
    Authors: Buznikov Et al.
    Exp Neurol 2010;32:43101
  24. Effects of TRPV1 activation on synaptic excitation in the dentate gyrus of a mouse model of temporal lobe epilepsy.
    Authors: Bhaskaran and Smith
    Br J Pharmacol 2010;223:529
  25. Reduction in endocannabinoid tone is a homeostatic mechanism for specific inhibitory synapses.
    Authors: Kim and Alger
    Nat Neurosci 2010;13:592
  26. Endocannabinoid-dependent LTD in a nociceptive synapse requires activation of a presynaptic TRPV-like receptor.
    Authors: Yuan and Burrell
    J Neurophysiol 2010;104:2766
  27. TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons.
    Authors: Gibson Et al.
    Neuron 2008;57:746
  28. Control of excitatory synaptic transmission by capsaicin is unaltered in TRPV1 vanilloid receptor knockout mice.
    Authors: Benninger Et al.
    J Pharmacol Exp Ther 2008;52:89
  29. Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic dopamine neurons through nuclear receptors.
    Authors: Melis Et al.
    J Neurosci 2008;28:13985
  30. Anandamide mediates hyperdynamic circulation in cirrhotic rats via CB(1) and VR(1) receptors.
    Authors: Moezi Et al.
    J Pharmacol Exp Ther 2006;149:898
  31. 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.
    Authors: Gavva Et al.
    J Pharmacol Exp Ther 2005;313:474
  32. Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats.
    Authors: Kwolek Et al.
    Br J Pharmacol 2005;145:567
  33. Pungent products from garlic activate the sensory ion channel TRPA1.
    Authors: Bautista Et al.
    Br J Pharmacol 2005;102:12248
  34. Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons.
    Authors: Price Et al.
    Br J Pharmacol 2004;142:257
  35. Anandamide acts as a vasodilator of dural blood vessels in vivo by activating TRPV1 receptors.
    Authors: Akerman Et al.
    Br J Pharmacol 2004;142:1354
  36. 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.
    Authors: Akerman Et al.
    Sci Rep 2003;140:718
  37. A possible role of lipoxygenase in the activation of vanilloid receptors by anandamide in the guinea-pig bronchus.
    Authors: Craib Et al.
    Mol Pharmacol 2001;134:42581
Expand to show all 37 Citations

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