The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain.
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.
Herdon
H
H
Department of Psychiatry Research, SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.
Jerman
J
J
Stean
T
T
Chan
W
W
Middlemiss
D
D
Upton
N
N
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*
D000927:Anticonvulsants; D001549:Benzamides; D001578:Benzopyrans; C102319:SB 204269