title: Anticonvulsant evaluation and mechanism of action of benzylamino enaminones.
abstract: 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.
authors.affiliation: Faculty of Pharmacy, Kuwait University, PO Box 24923, Safat 13110, Kuwait. ivanoe@hsc.edu.kw
authors.forename: Ivan O
authors.initials: IO
authors.lastname: Edafiogho
authors.forename: Kethireddy V V
authors.initials: KV
authors.lastname: Ananthalakshmi
authors.forename: Samuel B
authors.initials: SB
authors.lastname: Kombian
mesh_terms: 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
chemical_list: D000927:Anticonvulsants; D001596:Benzylamines; D003509:Cyclohexanecarboxylic Acids; D003510:Cyclohexanes; C082303:methyl 4-(benzylamino)-6-methyl-2-oxocyclohex-3-en-1-oate