Herdon H, Jerman J, Stean T, Chan W, Middlemiss D, Upton N
Department of Psychiatry Research, SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.
Eur J Pharmacol. 1996 Oct 31;314(3):R7-8. doi: 10.1016/s0014-2999(96)00737-6.
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.
新型化合物SB 204269（反式-(+)-6-乙酰基-4S-(4-氟苯甲酰氨基)-3,4-二氢-2,2-二甲基-2H-苯并[b]吡喃-3R-醇，半水合物）在小鼠最大电休克惊厥阈值试验中显示出强效抗惊厥活性。[3H]SB 204269与小鼠前脑细胞膜的结合具有饱和性（Bmax为217 fmol/mg蛋白质，Kd为32 nM）且具有立体特异性。SB 204269出色的抗惊厥谱，以及该化合物独特结合位点的确定，表明它作为癫痫的新型治疗方法具有潜在的临床应用价值。
