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Potent, 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).
Sold for research purposes under agreement from GlaxoSmithKline
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 287.75. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.48 mL||17.38 mL||34.75 mL|
|5 mM||0.7 mL||3.48 mL||6.95 mL|
|10 mM||0.35 mL||1.74 mL||3.48 mL|
|50 mM||0.07 mL||0.35 mL||0.7 mL|
References are publications that support the biological activity of the product.
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
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
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Keywords: SB 366791, SB 366791 supplier, Potent, selective, competitive, TRPV1, VR1, antagonists, Vanillioids, Receptors, TRPV, Channels, Transient, Receptor, Potential, SB366791, GlaxoSmithKline, GSK, 1615, Tocris Bioscience
14 Citations for SB 366791
Citations are publications that use Tocris products. Selected citations for SB 366791 include:
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
Li et al (2015) The Cancer Chemotherapeutic PacT. Increases Human and Rodent Sensory Neuron Responses to TRPV1 by Activation of TLR4. J Neurosci 35 13487 PMID: 26424893
Ambrosino et al (2013) Activation and desensitization of TRPV1 channels in sensory neurons by the PPARα agonist palmitoylethanolamide. Br J Pharmacol 168 1430 PMID: 23083124
Schuelert et al (2010) Paradoxical effects of the cannabinoid CB2 receptor agonist GW405833 on rat osteoarthritic knee joint pain. Osteoarthritis Cartilage 18 1536 PMID: 20863899
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
Graham et al (2013) Epidermal keratinocyte polarity and motility require Ca2+ influx through TRPV1. J Cell Sci 126 4602 PMID: 23943873
Hazari et al (2011) TRPA1 and sympathetic activation contribute to increased risk of triggered cardiac arrhythmias in hypertensive rats exposed to diesel exhaust. Environ Health Perspect 119 951 PMID: 21377951
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
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
Nguyen et al (2014) Transient receptor potential vanilloid type 1 channel may modulate opioid reward. Neuropsychopharmacology 39 2414 PMID: 24732880
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
Alvarez-Berdugo et al (2014) Pharmacodynamics of TRPV1 agonists in a bioassay using human PC-3 cells. ScientificWorldJournal 2014 184526 PMID: 24688365
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
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.