Cat. No. 1615
Chemical Name: 4'-Chloro-3-methoxycinnamanilide
Biological ActivityPotent, selective and competitive vanilloid TRPV1 receptor antagonist (pA2 = 7.71 at hVR1); antagonizes hTRPV1 receptors activated by agonists, noxious heat, but not protons. Displays selectivity over a wide range of receptors and systems including CB1 and CB2 receptors, voltage-gated Ca2+ channels and the hyperpolarization-activated current (Ih). Also available as part of the Vanilloid TRPV1 Receptor Tocriset™.
Licensing InformationSold for research purposes under agreement from GlaxoSmithKline
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 / Product Datasheet / Safety Data Sheet
Gavva et al (2005) Proton activation does not alter antagonist interaction with the capsaicin-binding pocket of TRPV1. Mol.Pharmacol. 68 1524. PMID: 16135784.
Gunthorpe et al (2004) Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Neuropharmacology 46 133. PMID: 14654105.
Fowler et al (2003) Inhibition of C6 glioma cell proliferation by anandamide, 1-arachidonylglycerol, and by a water soluble phosphate ester of anandamide: variability in response and involvement of arachidonic acid. Biochem.Pharmacol. 66 757. PMID: 12948856.
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Citations are publications that use Tocris products. Selected citations for SB 366791 include:
Nguyen et al (2014) Transient receptor potential vanilloid type 1 channel may modulate opioid reward. Neuropsychopharmacology 39 2414. PMID: 24732880.
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.
Shabir et al (2013) Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium. Mol Pain 305 F396. PMID: 23720349.
Casarotto et al (2012) 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. Am J Physiol Renal Physiol 37 478. PMID: 21937980.
Westlund et al (2010) Impact of central and peripheral TRPV1 and ROS levels on proinflammatory mediators and nociceptive behavior. J Biol Chem 6 46. PMID: 20691059.
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.
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.
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.
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Keywords: SB 366791, supplier, Potent, selective, competitive, TRPV1, VR1, antagonists, Vanillioids, Receptors, TRPV, Channels, Transient, Receptor, Potential, SB366791, GlaxoSmithKline, GSK, Tocris Bioscience, TRPV Antagonist products
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