Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C20H20FNO4 |
Molecular Weight | 357.3755 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(=O)C1=CC2=C(OC(C)(C)[C@H](O)[C@H]2NC(=O)C3=CC=C(F)C=C3)C=C1
InChI
InChIKey=RCLXAPJEFHPYEG-ZWKOTPCHSA-N
InChI=1S/C20H20FNO4/c1-11(23)13-6-9-16-15(10-13)17(18(24)20(2,3)26-16)22-19(25)12-4-7-14(21)8-5-12/h4-10,17-18,24H,1-3H3,(H,22,25)/t17-,18+/m0/s1
Molecular Formula | C20H20FNO4 |
Molecular Weight | 357.3755 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/12387702Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/9283703 | https://www.ncbi.nlm.nih.gov/pubmed/19443931 | https://www.ncbi.nlm.nih.gov/pubmed/15115635
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12387702
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/9283703 | https://www.ncbi.nlm.nih.gov/pubmed/19443931 | https://www.ncbi.nlm.nih.gov/pubmed/15115635
Carabersat is an anticonvulsant devoid of cardiovascular side effects with minimal central nervous system adverse actions. Carabersat does not bind to ion channels, purinergic, aminergic, opioid and other peptidergic receptors. It selectively interacts with its own binding site, which is not yet elucidated. Carabersat has no effect on sodium channels, GABAergic or glutamate pathways. Carabersat had been in phase II clinical trials for the treatment of epilepsy. It has a potential action in preventing migraines because it acts through an inhibition of the cortical spreading depression trigeminal nerve-induced vasodilatation in cats. Its good therapeutic index and the markedly reduced neurological impairments could make it a useful agent for migraine prophylaxis pending efficacy parameters of controlled studies, which are underway.
CNS Activity
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9283703
Rats: 1-30 mg/kg
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8957267
The binding of [3H]SB 204269 (Carabersat) to mouse forebrain membranes is saturable (Bmax 217 fmol/mg protein, Kd 32 nM) and stereospecific.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:22:09 GMT 2023
by
admin
on
Fri Dec 15 16:22:09 GMT 2023
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Record UNII |
K9R83652CK
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Record Status |
Validated (UNII)
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Record Version |
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-
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NCI_THESAURUS |
C264
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DTXSID6047319
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7764
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K9R83652CK
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193943
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CHEMBL39933
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300000034115
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C77999
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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SOLVATE->ANHYDROUS |
Related Record | Type | Details | ||
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ACTIVE MOIETY |