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Biological Activity for A 784168
A 784168 is a 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.
Compound Libraries for A 784168
Technical Data for A 784168
|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.
Solubility Data for A 784168
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for A 784168
The following data is based on the product molecular weight 479.4. 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||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 for A 784168
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
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1 Citation for A 784168
Citations are publications that use Tocris products. Selected citations for A 784168 include:
Alharris et al (2019) Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget 10 45 PMID: 30713602
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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.