Orally effective vanilloid receptor 1 (TRPV1 receptor) antagonist. Inhibits acid- and capsaicin-induced activation of rat TRPV1 receptors (IC50 values are 6.0 and 35 nM respectively). Displays analgesic properties in rat models of inflammatory and neuropathic pain. CNS penetrant.
|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 372.89. 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||2.68 mL||13.41 mL||26.82 mL|
|5 mM||0.54 mL||2.68 mL||5.36 mL|
|10 mM||0.27 mL||1.34 mL||2.68 mL|
|50 mM||0.05 mL||0.27 mL||0.54 mL|
References are publications that support the products' biological activity.
Pomonis et al (2003) N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: II. In vivo characterization in rat models of inflamma J.Pharmacol.Exp.Ther. 306 387 PMID: 12721336
Valenzano et al (2003) N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. In vitro characterization and pharmacokinetic proper J.Pharmacol.Exp.Ther. 306 377 PMID: 12721338
If you know of a relevant reference for BCTC, please let us know.
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Keywords: BCTC, supplier, vanilloid, trpv1, antagonists, transient, receptors, potential, channels, TRPV, TRPV, 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.