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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
Structure of JNJ-17203212

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)

HIDE SMILES / InChI
Molecular Formula C17H15F6N5O
Molecular Weight 419.3243
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
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

CNS Active
3913
Curator's Comment: JNJ-17203212 is CNS active in rodents. No human data available.

Originator

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 65.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Preclinical
Unknown

Approved Use

Unknown
Primary
Basic research
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
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
Two TRPV1 receptor antagonists are effective in two different experimental models of migraine.
2015
Patents

Patents

WO2010092342A1
1
WO2016127085A1
1
WO2016180543A1
1

Sample Use Guides

In Vivo Use Guide
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
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
Substance Class Chemical
Created
by admin
on Sat Dec 16 08:36:14 GMT 2023
Edited
by admin
on Sat Dec 16 08:36:14 GMT 2023
Record UNII
71JE0C439X
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
JNJ-17203212
Common Name English
1-PIPERAZINECARBOXAMIDE, 4-(3-(TRIFLUOROMETHYL)-2-PYRIDINYL)-N-(5-(TRIFLUOROMETHYL)-2-PYRIDINYL)-
Systematic Name English
4-(3-TRIFLUOROMETHYL)PYRIDIN-2-YL)PIPERAZINE-1-CARBOXYLIC ACID (5-(TRIFLUOROMETHYL)PYRIDIN-2-YL)AMIDE
Systematic Name English
Code System Code Type Description
PUBCHEM
11339118
Created by admin on Sat Dec 16 08:36:14 GMT 2023 , Edited by admin on Sat Dec 16 08:36:14 GMT 2023
PRIMARY
CAS
821768-06-3
Created by admin on Sat Dec 16 08:36:14 GMT 2023 , Edited by admin on Sat Dec 16 08:36:14 GMT 2023
PRIMARY
FDA UNII
71JE0C439X
Created by admin on Sat Dec 16 08:36:14 GMT 2023 , Edited by admin on Sat Dec 16 08:36:14 GMT 2023
PRIMARY
EPA CompTox
DTXSID50462856
Created by admin on Sat Dec 16 08:36:14 GMT 2023 , Edited by admin on Sat Dec 16 08:36:14 GMT 2023
PRIMARY
Related Record Type Details
Structure of JNJ-17203212
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