Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H15ClN4 |
| Molecular Weight | 322.792 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CN2N=C(C3=CC=C(N)C=C3)C4=CC(Cl)=CC=C4CC2=N1
InChI
InChIKey=FPXVCCSOTAQPIV-UHFFFAOYSA-N
InChI=1S/C18H15ClN4/c1-11-10-23-17(21-11)8-13-2-5-14(19)9-16(13)18(22-23)12-3-6-15(20)7-4-12/h2-7,9-10H,8,20H2,1H3
| Molecular Formula | C18H15ClN4 |
| Molecular Weight | 322.792 |
| 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/16203001 | https://www.ncbi.nlm.nih.gov/pubmed/14570761
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/16203001 | https://www.ncbi.nlm.nih.gov/pubmed/14570761
GYKI-472611 is a non-competitive AMPA antagonist receptor. Also, GYKI-47261 was considered as a potent CYP2E1 inducer. In vivo, it displays broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-472611 developed by IVAX Drug Research Institute Ltd. for treatment of epilepsy and parkinsonism.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2096670 |
2.3 µM [IC50] | ||
Target ID: CHEMBL2109241 |
4.5 µM [IC50] | ||
Target ID: CHEMBL5281 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Combined blockade of AMPA and NMDA glutamate receptors reduces levodopa-induced motor complications in animal models of PD. | 2005-12 |
|
| GYKI-47261, a new AMPA [2-amino-3-(3-hydroxymethylisoxazole-4-yl)propionic acid] antagonist, is a CYP2E1 inducer. | 2003-11 |
|
| New non competitive AMPA antagonists. | 2000-08 |
Patents
Sample Use Guides
The volumes of administration were 0.1 mL/10 g and 0.5 mL/100 g body weight for mice and rats, respectively and 6 mg/kg intravenous.
Route of Administration:
Other
During the 72-h exposure, GYKI-47261 was able to prevent or slow down the loss of CYP2E1 activity; however, the cells treated with GYKI-47261 for 72 h showed somewhat lower chlorzoxazone 6-hydroxylase activity than did freshly isolated hepatocytes. Although CYP2E1 mRNA of the cultured cells rapidly decreased, a small amount (about 6% of the initial level) was detected in GYKI-47261-treated (10 and 50 uM) cells at 48 h.
| Substance Class |
Chemical
Created
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Edited
Wed Apr 02 10:25:56 GMT 2025
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| Record UNII |
05588G41R2
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| Record Status |
Validated (UNII)
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| Record Version |
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