Anticonvulsant evaluation and mechanism of action of benzylamino enaminones

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 (ED50) 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.

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.Figure optionsDownload as PowerPoint slide