Anticonvulsant evaluation and mechanism of action of benzylamino enaminones

Anticonvulsant evaluation and electrophysiology data suggest that the anticonvulsant benzylamino enaminones inhibit a glutamate machinery and action potential firing in the central nervous system to produce their effects. The mechanism of anticonvulsant action was evaluated for the benzylamino enami...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2006-08, Vol.14 (15), p.5266-5272
Main Authors: Edafiogho, Ivan O., Ananthalakshmi, Kethireddy V.V., Kombian, Samuel B.
Format: Article
Language:English
Subjects:
Action Potentials - drug effects
Administration, Oral
Animals
Anticonvulsants
Anticonvulsants - chemistry
Anticonvulsants - pharmacology
Anticonvulsants. Antiepileptics. Antiparkinson agents
Benzylamines - chemistry
Benzylamines - pharmacology
Benzylamines - therapeutic use
Biological and medical sciences
Cells, Cultured
Cyclohexanecarboxylic Acids
Cyclohexanes - chemistry
Cyclohexanes - therapeutic use
Dose-Response Relationship, Drug
Drug Evaluation, Preclinical
Electrophysiology
Enaminones
Excitatory Postsynaptic Potentials - drug effects
Male
Mechanism
Medical sciences
Mice
Mice, Inbred Strains
Molecular Structure
Neurons - drug effects
Neuropharmacology
Nucleus Accumbens - cytology
Pharmacology. Drug treatments
QSAR
Quantitative Structure-Activity Relationship
Rats
Rats, Sprague-Dawley
Seizures - drug therapy
Seizures - prevention & control
Stereoisomerism
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Summary:Anticonvulsant evaluation and electrophysiology data suggest that the anticonvulsant benzylamino enaminones inhibit a glutamate machinery and action potential firing in the central nervous system to produce their effects. The mechanism of anticonvulsant action was evaluated for the benzylamino enaminones. The most potent enaminone in this series was the unsubstituted benzylamine analog ( 30; methyl 4-benzylamino-6-methyl-2-oxocyclohex-3-en-1-oate) which had an oral effective dose (ED 50) in rats of 27 mg/kg against maximal electroshock seizures, and a concentration 10-fold less than this dose depressed excitatory synaptic transmission, and action potential firing in the rat brain in vitro.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2006.03.049