作者:J.R. Dimmock、S.S. Jonnalagadda、O.A. Phillips、E. Erciyas、K. Shyam、H.A. Semple
DOI:10.1002/jps.2600810509
日期:1992.5
prepared revealed that many had activity comparable with that of clinically useful drugs in the MES screen. The anticonvulsant properties of eight of the compounds following oral administration were reduced considerably or abolished compared with those following intraperitoneal administration. Various synthetic strategies for future development of potential anticonvulsants are outlined.
制备了三十种1-芳基-5-二甲基氨基-1-戊烯-3-氢卤化物和相关化合物作为候选抗惊厥药,并在最大电击发作(MES),皮下戊四氮阈值和神经毒性筛查中进行了评估。通过腹膜内途径给药后,许多化合物在MES筛选中均具有活性,而仅10%的曼尼希碱在皮下戊四唑测试中提供了保护。定量制备的一半化合物表明,在MES筛查中,许多化合物的活性与临床上有用的药物相当。与腹膜内给药相比,口服给药后的八种化合物的抗惊厥特性大大降低或消失。