Cat. No. 3361
Chemical Name: 4-[3-(Trifluoromethyl)-2-pyridinyl]
Biological ActivityReversible, 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.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
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.
Ghilardi et al (2005) Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J.Neurosci. 25 3126. PMID: 15788769.
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.
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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.
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Keywords: JNJ 17203212, supplier, Reversible, competitive, potent, TRPV1, antagonists, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, JNJ17203212, Tocris Bioscience, TRPV Antagonist products