Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H19N5OS |
| Molecular Weight | 365.452 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C(NC1=CC=CC=C1)N2CCN(CC2)C3=NC(=NS3)C4=CC=CC=C4
InChI
InChIKey=BHBOSTKQCZEAJM-UHFFFAOYSA-N
InChI=1S/C19H19N5OS/c25-18(20-16-9-5-2-6-10-16)23-11-13-24(14-12-23)19-21-17(22-26-19)15-7-3-1-4-8-15/h1-10H,11-14H2,(H,20,25)
| Molecular Formula | C19H19N5OS |
| Molecular Weight | 365.452 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/19095868 | https://www.ncbi.nlm.nih.gov/pubmed/18693015 | https://www.ncbi.nlm.nih.gov/pubmed/27318096 | https://www.ncbi.nlm.nih.gov/pubmed/27899300 | https://www.ncbi.nlm.nih.gov/pubmed/26567045
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/19095868 | https://www.ncbi.nlm.nih.gov/pubmed/18693015 | https://www.ncbi.nlm.nih.gov/pubmed/27318096 | https://www.ncbi.nlm.nih.gov/pubmed/27899300 | https://www.ncbi.nlm.nih.gov/pubmed/26567045
JNJ-1661010 is a potent and selective is a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. FAAH is a membrane bound serine hydrolase primarily responsible for the breakdown of the endogenous cannabinoid anandamide in the CNS. Increasing the amount of anandamide, which has analgesics properties, may be efficacious in the treatment of pain. According to the experimental data JNJ-1661010 may be useful clinically as broad-spectrum analgesics. Johnson & Johnson is developing JNJ-1661010 for the treatment of neuropathic pain. Preclinical development is being conducted in the US. In addition recent data demonstrated that JNJ-1661010 could be useful in the treatment of arthritis and parkinson's disease. JNJ-1661010 inhibits myometrial contractility, without un-specific relaxing effects on the smooth muscle.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19095868 | https://www.ncbi.nlm.nih.gov/pubmed/27318096
Curator's Comment: JNJ-1661010 is CNS active in rodents. No human data available.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2243 |
33.0 nM [IC50] | ||
Target ID: CHEMBL1628475 |
5.7 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Role of the endocannabinoid system in the control of mouse myometrium contractility during the menstrual cycle. | 2017-01-15 |
|
| Fatty acid amide hydrolase inhibition for the symptomatic relief of Parkinson's disease. | 2016-10 |
|
| Anti-inflammatory effects of N-acylethanolamines in rheumatoid arthritis synovial cells are mediated by TRPV1 and TRPA1 in a COX-2 dependent manner. | 2015-11-14 |
|
| Dynamic regulation of the endocannabinoid system: implications for analgesia. | 2009-10-08 |
|
| Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. | 2009-01 |
|
| Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. | 2008-09-01 |
Sample Use Guides
20 mg/kg JNJ-1661010 exerts potent analgetic action in rats.
Mice were injected daily with JNJ1661010 (20 mg/kg) reduced arthritis score.
Route of Administration:
Intraperitoneal
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 22:09:59 GMT 2025
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Mon Mar 31 22:09:59 GMT 2025
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| Record UNII |
62521S57AU
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| Record Status |
Validated (UNII)
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| Record Version |
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