title: Effect of gamma-decanolactone on glutamate binding in the rat cerebral cortex.
abstract: Epilepsy is one of the most common neurological disorders. Even though antiepileptic drugs can afford a reasonably satisfactory treatment for 80% of diagnosed patients, chronic intractable epilepsy still affects a significant number of people and more effective and less harmful antiepileptic drugs are needed. Previous studies have shown that gamma-decanolactone has dose-dependent sedative effects, including hypnotic, anticonvulsant and hypothermic properties in mice. The present study reports an inhibitory effect of gamma-decanolactone on glutamate binding (96.8% with 5 mM) in rat cortex membranes. The non competitive nature of glutamate binding inhibition as a neurochemical correlate of the anticonvulsant activity of gamma-decanolactone may be a relevant mode of action for further drug development.
authors.affiliation: Departamento de Farmacologia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil.
authors.forename: P
authors.initials: P
authors.lastname: Pereira
authors.forename: E
authors.initials: E
authors.lastname: Elisabetsky
authors.forename: D O
authors.initials: DO
authors.lastname: Souza
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D007700:Kinetics; D007783:Lactones / Q000494:pharmacology*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D017470:Receptors, Glutamate / Q000187:drug effects* / Q000378:metabolism
chemical_list: D000927:Anticonvulsants; D007783:Lactones; D017470:Receptors, Glutamate; C109757:decan-4-olide