Potent TRPV1 antagonist (IC50 = 3-9 nM). Blocks capsaicin-evoked currents in rat DRG neurons and inhibits TRPV1-activation by anandamide (Cat. No. 1339) and N-arachidonoyl-dopamine. Reduces pain in inflammatory, postoperative and osteoarthritic in vivo pain models.
|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 345.32. 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||2.9 mL||14.48 mL||28.96 mL|
|5 mM||0.58 mL||2.9 mL||5.79 mL|
|10 mM||0.29 mL||1.45 mL||2.9 mL|
|50 mM||0.06 mL||0.29 mL||0.58 mL|
References are publications that support the biological activity of the product.
El Kouhen et al (2005) A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid. J.Pharmacol.Exp.Ther. 314 400 PMID: 15837819
McGaraughty et al (2006) Systemic and site-specific effects of A-425619, a selective TRPV1 receptor antagonist, on wide dynamic range neurons in CFA-treated and uninjured rats. J.Neurophysiol. 95 18 PMID: 16162831
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Keywords: A 425619, A 425619 supplier, A425619, TRPV1, antagonists, antagonism, transient, receptor, potential, channels, vanilloids, pain, nociception, capsaicin, TRPV, 5781, Tocris Bioscience
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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.