Chapman A G, Graham J, Meldrum B S
Department of Neurology, Institute of Psychiatry, De Crespigny Park, London, U.K.
Eur J Pharmacol. 1990 Mar 13;178(1):97-9. doi: 10.1016/0014-2999(90)94798-3.
CPP (3-(2-carboxypiperazine-4-yl)-1-phosphonate), and its unsaturated analogue, CPPene (3-(2-carboxypiperazine-4-yl)-1-propenyl-1-phosphonic acid), have potent anticonvulsant activity against sound-induced clonic seizures in DBA/2 mice. Following i.p. administration the protection is maximal at 1-2 h, and the ED50 values (mumol/kg) are: D(-)-CPPene, 1.54; D(-)-CPP, 2.75; D,L( +/- )-CPP, 4.36. Following oral administration the protection is maximal at 3-4 h and the ED50 (mumol/kg) values are: D(-)-CPPene, 40.19; D(-)-CPP, 65.80; D,L( +/- )-CPP, 108.1.
CPP（3-（2-羧基哌嗪-4-基）-1-膦酸）及其不饱和类似物CPPene（3-（2-羧基哌嗪-4-基）-1-丙烯基-1-膦酸）对DBA/2小鼠的声音诱发阵挛性惊厥具有强大的抗惊厥活性。腹腔注射给药后，1-2小时时保护作用最强，半数有效剂量（μmol/kg）值分别为：D（-）-CPPene，1.54；D（-）-CPP，2.75；消旋CPP，4.36。口服给药后，3-4小时时保护作用最强，半数有效剂量（μmol/kg）值分别为：D（-）-CPPene，40.19；D（-）-CPP，65.80；消旋CPP，108.1。
