Borenstein M R, Doukas P H
J Pharm Sci. 1987 Apr;76(4):300-2. doi: 10.1002/jps.2600760407.
A series of Mannich bases derived from spiro [indan-1,3'pyrrolidine-2',5'-dione] were evaluated for anticonvulsant activity. This activity varied as a function of the amine substituent and several compounds showed protective effects in both the maximal electroshock (MES) and subcutaneous pentylenetetrazol (scMet) assays. In addition, fluorenyl- and cyclopentyl-derived spirosuccinimides, as well as extended chain analogues, were tested and proved to be inactive. A time versus effect study was conducted employing the MES assay and the hydroxyethylpiperazine-derived Mannich base of spiro [indan-1,3 pyrrolidine-2',5',dione]. This compound acted rapidly and its protective half-life was increased as larger doses were administered.
对一系列源自螺[茚满-1,3'-吡咯烷-2',5'-二酮]的曼尼希碱进行了抗惊厥活性评估。该活性随胺取代基的变化而变化，几种化合物在最大电休克（MES）和皮下注射戊四氮（scMet）试验中均显示出保护作用。此外，对芴基和环戊基衍生的螺琥珀酰亚胺以及长链类似物进行了测试，结果证明它们没有活性。采用MES试验对螺[茚满-1,3-吡咯烷-2',5',二酮]的羟乙基哌嗪衍生的曼尼希碱进行了时间-效应研究。该化合物起效迅速，随着给药剂量的增加，其保护半衰期延长。
