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.