Catalog Number: 3361
Chemical Name: 4-[3-(Trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinecarboxamide
Biological Activity
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.
Technical Data
  • M.Wt:
    419.32
  • Formula:
    C17H15F6N5O
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    821768-06-3
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.
Background References
  1. 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.
    Swanson et al.
    J.Med.Chem., 2005;48:1857
  2. Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain.
    Ghilardi et al.
    J.Neurosci., 2005;25:3126
  3. 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.
    Bhattacharya et al.
    J.Pharmacol.Exp.Ther., 2007;323:665
Citations:

The citations listed below are publications that use Tocris products. Selected citations for JNJ 17203212 include:

2 Citations: Showing 1 - 2
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  1. Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain.
    Authors: Kelly Et al.
    PLoS One 2015;74:252
  2. Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers.
    Authors: Vijayvergiya Et al.
    PLoS One 2015;10:e0141366

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