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.
Edafiogho
Ivan O
IO
Faculty of Pharmacy, Kuwait University, PO Box 24923, Safat 13110, Kuwait. ivanoe@hsc.edu.kw
Ananthalakshmi
Kethireddy V V
KV
Kombian
Samuel B
SB
D000200:Action Potentials / Q000187:drug effects; D000284:Administration, Oral; D000818:Animals; D000927:Anticonvulsants / Q000737:chemistry / Q000494:pharmacology*; D001596:Benzylamines / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D002478:Cells, Cultured; D003509:Cyclohexanecarboxylic Acids; D003510:Cyclohexanes / Q000737:chemistry / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D004594:Electrophysiology; D019706:Excitatory Postsynaptic Potentials / Q000187:drug effects; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D015394:Molecular Structure; D009474:Neurons / Q000187:drug effects; D009714:Nucleus Accumbens / Q000166:cytology; D021281:Quantitative Structure-Activity Relationship; D051381:Rats; D017207:Rats, Sprague-Dawley; D012640:Seizures / Q000188:drug therapy / Q000517:prevention & control; D013237:Stereoisomerism
D000927:Anticonvulsants; D001596:Benzylamines; D003509:Cyclohexanecarboxylic Acids; D003510:Cyclohexanes; C082303:methyl 4-(benzylamino)-6-methyl-2-oxocyclohex-3-en-1-oate