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)
DescriptionSources: http://adisinsight.springer.com/drugs/800021451Curator'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
Sources: http://adisinsight.springer.com/drugs/800021451
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4794 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15771431 |
65.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17690251 |
Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Overexpressed transient receptor potential vanilloid 3 ion channels in skin keratinocytes modulate pain sensitivity via prostaglandin E2. | 2008 Dec 17 |
|
Selective pharmacological blockade of the TRPV1 receptor suppresses sensory reflexes of the rodent bladder. | 2009 Aug |
|
Transient receptor potential channels mediate the tussive response to prostaglandin E2 and bradykinin. | 2012 Oct |
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22790593
Preincubation with the 1uM JNJ-17203212 inhibited the increase in mRNA for lyso-PAF AT, IL-8, eotaxin 1, -2, and -3, MCP-1, and MIP-1α in ATP in HCl-stimulated HET-1A cells
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ACTIVE MOIETY