Capsazepine

  ( 50 citations )    
Product Datasheet
Catalog Number:0464
Chemical Name:N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide
Product Details
Citations (50)
Supplemental Products
Reviews
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.
Product Datasheets
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Citations:

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

50 Citations: Showing 1 - 10
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  1. AM404, paracetamol metabolite, prevents prostaglandin synthesis in activated microglia by inhibiting COX activity.
    Authors: Saliba
    J Neuroinflammation  2017;14(1):246
  2. 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
  3. 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
  4. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent.
    Authors: Borrelli Et al.
    PLoS One  2015;172:142
  5. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    J Neurosci  2015;16:5555
  6. Experimental evidence for alleviating nociceptive hypersensitivity by single application of capsaicin.
    Authors: Ma Et al.
    Mol Pain  2015;11:22
  7. Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers.
    Authors: Vijayvergiya Et al.
    PLoS One  2015;10:e0141366
  8. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
    Authors: Smith Et al.
    PLoS One  2015;10:e0136546
  9. 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
  10. Transient receptor potential vanilloid type 1 channel may modulate opioid reward.
    Authors: Nguyen Et al.
    Neuropsychopharmacology  2014;39:2414
  11. 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
  12. 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
  13. 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
  14. Dexamethasone rapidly increases GABA release in the dorsal motor nucleus of the vagus via retrograde messenger-mediated enhancement of TRPV1 activity.
    Authors: Derbenev and Smith
    PLoS One  2013;8:e70505
  15. CB1 cannabinoid receptors couple to focal adhesion kinase to control insulin release.
    Authors: Malenczyk Et al.
    J Biol Chem  2013;288:32685
  16. Epidermal keratinocyte polarity and motility require Ca2+ influx through TRPV1.
    Authors: Graham Et al.
    J Cell Sci  2013;126:4602
  17. The cytochrome P450 inhibitor, ketoconazole, inhibits oxidized linoleic acid metabolite-mediated peripheral inflammatory pain.
    Authors: Ruparel Et al.
    Mol Pain  2012;8:73
  18. 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
  19. Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH.
    Authors: Kaszás Et al.
    Dev Neurosci  2012;340:152
  20. Ischemic neuroprotection by TRPV1 receptor-induced hypothermia.
    Authors: Muzzi Et al.
    Br J Pharmacol  2012;32:978
  21. The association of N-palmitoylethanolamine with the FAAH inhibitor URB597 impairs melanoma growth through a supra-additive action.
    Authors: Hamtiaux Et al.
    BMC Cancer  2012;12:92
  22. 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
  23. TRPV4 channels mediate the infrared laser-evoked response in sensory neurons.
    Authors: Albert Et al.
    J Neurophysiol  2012;107:3227
  24. 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
  25. Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism.
    Authors: Hamtiaux Et al.
    PLoS One  2011;6:e26823
  26. 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
  27. Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms.
    Authors: Li and Burrell
    Learn Mem  2011;18:545
  28. Post-ictal analgesia in genetically epilepsy-prone rats is induced by audiogenic seizures and involves cannabinoid receptors in the periaqueductal gray.
    Authors: Samineni Et al.
    Brain Res  2011;1389:177
  29. A putative 'pre-nervous' endocannabinoid system in early echinoderm development.
    Authors: Buznikov Et al.
    Exp Neurol  2010;32:43101
  30. 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
  31. Reduction in endocannabinoid tone is a homeostatic mechanism for specific inhibitory synapses.
    Authors: Kim and Alger
    Nat Neurosci  2010;13:592
  32. Endocannabinoid-dependent LTD in a nociceptive synapse requires activation of a presynaptic TRPV-like receptor.
    Authors: Yuan and Burrell
    J Neurophysiol  2010;104:2766
  33. TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons.
    Authors: Gibson Et al.
    Neuron  2008;57:746
  34. 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
  35. Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic dopamine neurons through nuclear receptors.
    Authors: Melis Et al.
    J Neurosci  2008;28:13985
  36. Cannabinoid (CB1) receptor activation inhibits trigeminovascular neurons.
    Authors: Akerman Et al.
    J Pharmacol Exp Ther  2007;320:64
  37. Cannabinoids elicit antidepressant-like behavior and activate serotonergic neurons through the medial prefrontal cortex.
    Authors: Bambico Et al.
    J Neurosci  2007;27:11700
  38. 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
  39. 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
  40. Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats.
    Authors: Kwolek Et al.
    Br J Pharmacol  2005;145:567
  41. Pungent products from garlic activate the sensory ion channel TRPA1.
    Authors: Bautista Et al.
    Br J Pharmacol  2005;102:12248
  42. Endocannabinoids mediate presynaptic inhibition of glutamatergic transmission in rat ventral tegmental area dopamine neurons through activation of CB1 receptors.
    Authors: Melis Et al.
    J Neurosci  2004;24:53
  43. 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
  44. The cannabinomimetic arachidonyl-2-chloroethylamide (ACEA) acts on capsaicin-sensitive TRPV1 receptors but not cannabinoid receptors in rat joints.
    Authors: Baker
    Br J Pharmacol  2004;142:1361
  45. 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
  46. 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
  47. Synergistic interactions between airway afferent nerve subtypes mediating reflex bronchospasm in guinea pigs.
    Authors: Mazzone and Canning
    Am J Physiol Regul Integr Comp Physiol  2002;283:R86
  48. Characterization of the anandamide induced depolarization of guinea-pig isolated vagus nerve.
    Authors: Kagaya Et al.
    Br J Pharmacol  2002;137:39
  49. 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
  50. Effect of vanilloid drugs on gastrointestinal transit in mice.
    Authors: Izzo Et al.
    Br J Pharmacol  2001;132:1411
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VersaClone cDNA Plasmids
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Rat Vanilloid R1/TRPV1 (NP_114188) VersaClone cDNA

RDC1967
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