Abstract
The novel compound SB 204269 ( trans-(+)-6-acetyl-4 S-(4-fluorobenzoylamino)-3,4-dihydro-2,2-dimethyl-2 H-benzo[ b]pyran-3 R-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 ( B max 217 fmol/mg protein, K d 32 nM) and stereospecific. The excellent anticonvulsant profile of SB 204269, combined with the identification of a unique central binding site for the compound, suggest that it has potential clinical utility as a novel treatment for epilepsy.
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