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TRPV1 positive allosteric modulator. Potentiates vanilloid and proton activation of TRPV1 channels. Exhibits analgesic effects in combination with capsaicin (Cat. No. 0462) in rats. Also prolongs capsaicin-induced hypothermia in mice.
|Storage||Store at -20°C|
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 389.51. 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||2.57 mL||12.84 mL||25.67 mL|
|5 mM||0.51 mL||2.57 mL||5.13 mL|
|10 mM||0.26 mL||1.28 mL||2.57 mL|
|50 mM||0.05 mL||0.26 mL||0.51 mL|
References are publications that support the biological activity of the product.
Kaszas et al (2012) Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH. J.Pharmacol.Exp.Ther. 340 152 PMID: 22005042
Lebovitz et al (2012) Positive allosteric modulation of TRPV1 as a novel analgesic mechanism. Mol.Pain 8 PMID: 22998799
Roh et al (2008) Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1). Bioorg.Med.Chem. 16 9349 PMID: 18809334
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Keywords: MRS 1477, MRS 1477 supplier, MRS1477, TRPV1, transient, receptors, potential, channels, positive, allosteric, modulators, analgesic, PAM, TRPV, 5246, 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.