Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H12N2O.ClH |
Molecular Weight | 272.73 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.O=C(CN1C=CN=C1)C2=CC=C3C=CC=CC3=C2
InChI
InChIKey=DOBNXXMVNHWJKU-UHFFFAOYSA-N
InChI=1S/C15H12N2O.ClH/c18-15(10-17-8-7-16-11-17)14-6-5-12-3-1-2-4-13(12)9-14;/h1-9,11H,10H2;1H
Molecular Formula | C15H12N2O |
Molecular Weight | 236.2686 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Nafimidone is a candidate anticonvulsant agent. The anticonvulsant effectiveness of nafimidone was evaluated in the kindled amygdaloid seizure model in rats. Nafimidone (25-50 mg/kg) significantly reduced supranthreshold elicited afterdischarge length and seizure severity only at doses with some prestimulation toxicity. The maximum anticonvulsant effectiveness for the 25 mg/kg i.p. dose of nafimidone was seen between 15 and 30 min utilizing a suprathreshold kindling paradigm. Nafimidone did not significantly elevate seizure thresholds at the doses tested; however, nafimidone (3.1-50 mg/kg) reduced the severity and afterdischarge duration of threshold elicited seizures in a non-dose response manner. Nafimidone is a new antiepileptic drug which may be effective in partial onset seizures in humans.
Approval Year
Sample Use Guides
Rats: The absorption, distribution, excretion, and metabolism of 14C-nafimidone, a novel anticonvulsant, have been studied in rats. Nafimidone was completely absorbed following single oral doses of 10 and 100 mg/kg.
Humans, chronic intractable epilepsy: The half-life of nafimidone was 1.34 +/- 0.48 hours after a 100mg single dose and 1.69 +/- 0.91 hours after a 300mg single dose.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17786623
Curator's Comment: Inhibition of cytochrome P450(CYP)-selective reactions in a single human and a single mouse hepatic microsome preparation by fourteen 1-substituted imidazoles provides a simultaneous ranking of reaction susceptibility to a specific imidazole and the relative inhibitory potency of the imidazoles for a given reaction.
Nafimidone exhibited an IC(50) value <0.3 uM towards CYP2D6 and CYP1A2 reactions.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:07:08 GMT 2023
by
admin
on
Fri Dec 15 15:07:08 GMT 2023
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Record UNII |
LU0A7HD640
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C264
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CHEMBL416801
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C90708
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51199
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LU0A7HD640
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DTXSID40221116
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T-98
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70891-37-1
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