title: The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain.
abstract: The novel compound SB 204269 (trans-(+)-6-acetyl-4S-(4-fluorobenzoylamino)- 3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3R-ol, hemihydrate) shows potent anticonvulsant activity in the mouse maximal electroshock seizure threshold test. The binding of [3H]SB 204269 to mouse forebrain membranes is saturable (Bmax 217 fmol/mg protein, Kd 32 nM) and stereospecific. The excellent anticonvulsant profile of SB 204269, combined with the identification of a unique binding site for the compound, suggest that it has potential clinical utility as a novel treatment for epilepsy.
authors.affiliation: Department of Psychiatry Research, SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.
authors.forename: H
authors.initials: H
authors.lastname: Herdon
authors.forename: J
authors.initials: J
authors.lastname: Jerman
authors.forename: T
authors.initials: T
authors.lastname: Stean
authors.forename: W
authors.initials: W
authors.lastname: Chan
authors.forename: D
authors.initials: D
authors.lastname: Middlemiss
authors.forename: N
authors.initials: N
authors.lastname: Upton
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000378:metabolism*; D001549:Benzamides / Q000378:metabolism*; D001578:Benzopyrans / Q000378:metabolism*; D001665:Binding Sites; D008566:Membranes / Q000378:metabolism; D051379:Mice; D016548:Prosencephalon / Q000378:metabolism*
chemical_list: D000927:Anticonvulsants; D001549:Benzamides; D001578:Benzopyrans; C102319:SB 204269