Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C17H15F6N5O |
| Molecular Weight | 419.3243 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)(F)C1=CN=C(NC(=O)N2CCN(CC2)C3=NC=CC=C3C(F)(F)F)C=C1
InChI
InChIKey=JFRYYGVYCWYIDQ-UHFFFAOYSA-N
InChI=1S/C17H15F6N5O/c18-16(19,20)11-3-4-13(25-10-11)26-15(29)28-8-6-27(7-9-28)14-12(17(21,22)23)2-1-5-24-14/h1-5,10H,6-9H2,(H,25,26,29)
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/15771431 | https://www.ncbi.nlm.nih.gov/pubmed/17690251
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/15771431 | https://www.ncbi.nlm.nih.gov/pubmed/17690251
JNJ-17203212 is an TRPV1 receptor antagonist. The drug exerts potent antinociceptive and antitussive actions. JNJ-17203212 is developing by Johnson & Johnson for the treatment of pain and cough. No development reported.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15771431 | https://www.ncbi.nlm.nih.gov/pubmed/26109436
Curator's Comment: JNJ-17203212 is CNS active in rodents. No human data available.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Two TRPV1 receptor antagonists are effective in two different experimental models of migraine. | 2015 |
|
| Transient receptor potential channels mediate the tussive response to prostaglandin E2 and bradykinin. | 2012-10 |
|
| A novel TRPV1 receptor antagonist JNJ-17203212 attenuates colonic hypersensitivity in rats. | 2010-10 |
|
| Selective pharmacological blockade of the TRPV1 receptor suppresses sensory reflexes of the rodent bladder. | 2009-08 |
|
| Overexpressed transient receptor potential vanilloid 3 ion channels in skin keratinocytes modulate pain sensitivity via prostaglandin E2. | 2008-12-17 |
|
| 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. | 2007-11 |
|
| 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. | 2005-03-24 |
Sample Use Guides
rats: 24 µmol/kg JNJ-17203212 (ip, po) exerts antinociceptive action.
guinea pigs: 20 mg/kg (ip) JNJ-17203212 exerts antitussive action.
mice: 30 mg/kg JNJ-17203212 (sc) exerts antinociceptive action
Route of Administration:
Other
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ACTIVE MOIETY
