Potent TRPV1 antagonist (IC50 = 25 nM for inhibition of TRPV1 activation by 50 nM capsaicin). Displays no activity against a range of receptors, including TRPA1, GABA, opioid, and purinergic receptors.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 479.4. Batch specific molecular weights may vary from batch to batch due to solvent 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||2.09 mL||10.43 mL||20.86 mL|
|5 mM||0.42 mL||2.09 mL||4.17 mL|
|10 mM||0.21 mL||1.04 mL||2.09 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References are publications that support the biological activity of the product.
Bianchi et al (2007) [3H]-A-778317 [1-((R-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor. J.Pharmacol.Exp.Ther. 323 285 PMID: 17660385
Cui et al (2006) TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J.Neurosci. 26 9385 PMID: 16971522
If you know of a relevant reference for A 784168, please let us know.
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Literature in this Area
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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.