Reversible, competitive and potent TRPV1 antagonist (pKi values are 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively). Inhibits capsaicin- and H+-induced channel activation (pIC50 values are 6.32 and 7.23 respectively) and exhibits antitussive and analgesic activity in vivo.
|Storage||Store at +4°C|
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 419.32. 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||2.38 mL||11.92 mL||23.85 mL|
|5 mM||0.48 mL||2.38 mL||4.77 mL|
|10 mM||0.24 mL||1.19 mL||2.38 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
References are publications that support the products' biological activity.
Swanson et al (2005) Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J.Med.Chem. 48 1857 PMID: 15771431
Ghilardi et al (2005) Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J.Neurosci. 25 3126 PMID: 15788769
Bhattacharya et al (2007) Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs. J.Pharmacol.Exp.Ther. 323 665 PMID: 17690251
If you know of a relevant reference for JNJ 17203212, please let us know.
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Keywords: JNJ 17203212, supplier, Reversible, competitive, potent, TRPV1, antagonists, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, JNJ17203212, TRPV, TRPV, Tocris Bioscience
2 Citations for JNJ 17203212
Citations are publications that use Tocris products. Selected citations for JNJ 17203212 include:
Kelly et al (2015) Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain. PLoS One 74 252 PMID: 24152419
Vijayvergiya et al (2015) Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers. PLoS One 10 e0141366 PMID: 26513481
Do you know of a great paper that uses JNJ 17203212 from Tocris? If so please let us know.
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Literature in this Area
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.