Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C17H21N5OS |
| Molecular Weight | 343.447 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)C1=C2C(SC3=C2N=CN(N4CCCCCC4)C3=O)=NC=C1
InChI
InChIKey=GYWGXEGOXODOQU-UHFFFAOYSA-N
InChI=1S/C17H21N5OS/c1-20(2)12-7-8-18-16-13(12)14-15(24-16)17(23)22(11-19-14)21-9-5-3-4-6-10-21/h7-8,11H,3-6,9-10H2,1-2H3
| Molecular Formula | C17H21N5OS |
| Molecular Weight | 343.447 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/17016515 | http://adisinsight.springer.com/drugs/800024545Curator's Comment: Description was created based on several sources, includinghttps://www.ncbi.nlm.nih.gov/pubmed/17551319
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17016515 | http://adisinsight.springer.com/drugs/800024545
Curator's Comment: Description was created based on several sources, includinghttps://www.ncbi.nlm.nih.gov/pubmed/17551319
A-841720, a novel, potent and non-competitive mGluR1 antagonist in models of pain and of motor and cognitive function, is being under development by Merz Pharmaceuticals GmbH. It is a selective non-competitive mGlu1 receptor antagonist (IC50: 10 nM); showing 34-fold selectivity over mGluR5 and no significant activity at other mGluR receptors, neurotransmitter receptors, ion channels, and transporters. A-841720 demonstrated full efficacy in various in vivo animal pain models.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists. | 2005 Nov 17 |
|
| Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists. | 2006 Sep 15 |
|
| Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats. | 2008 Feb 12 |
Patents
Sample Use Guides
A-841720 significantly reduced formalin-induced behaviours,
such as hindpaw flinching and licking, at the doses
of 10 and 30 mg/kg
Route of Administration:
Intraperitoneal
| Substance Class |
Chemical
Created
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Sat Dec 16 10:04:13 GMT 2023
by
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| Record UNII |
U8C5C9D65S
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| Record Status |
Validated (UNII)
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| Record Version |
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