Belcheva I, Dimov S, Stoychev T
Acta Physiol Pharmacol Bulg. 1981;7(2):43-52.
The anticonvulsant properties of two N-aminomethyl derivatives of 3,3-diethyl-2,4-pyridinedione (persedon) are studied on two experimental models of generalized (pentylenetetrazol and penicillin) epilepsy in cats. N-aminomethylmorpholine 3,3-diethyl-2,4-pyridinedione (DKMM) applied in doses of 100 mg/ng i. v. in cases of pentylenetetrazol epilepsy leads to a rise in the convulsive thresholds (n, N) by 1.5 and two times, respectively. Administration of the drug in the same dose on developed penicillin epilepsy in cats reveals slight to moderate suppression of the generalized paroxysms, lasting until the 90th-120th min. N-aminomethylpiperazine 3,3-diethyl-2,4-pyridinedione (DKMP), injected in a dose of 100 mg/kg i. v., raises the pentylenetetrazol threshold ("n") 3.5 to 4 times and 8-10 times the N-threshold, approaching the effect of diazepam (10 mg/kg i. v.). On the background of injected DKMP it is difficult to attain epileptic status, and in the case of developed epileptic status DKMP in a dose of 50 mg/kg suppresses completely the seizure manifestations. Injection of DKMP in the cases of developed penicillin epilepsy results in complete suppression of the generalized paroxysmal activity, lasting until the 100th-120th min.
在猫的两种全身性（戊四氮和青霉素）癫痫实验模型上研究了3,3 - 二乙基 - 2,4 - 吡啶二酮（派西多）的两种N - 氨甲基衍生物的抗惊厥特性。在戊四氮癫痫情况下，静脉注射剂量为100mg/kg的N - 氨甲基吗啉3,3 - 二乙基 - 2,4 - 吡啶二酮（DKMM），可使惊厥阈值（n，N）分别提高1.5倍和两倍。在猫已发生的青霉素癫痫中以相同剂量给药，可发现全身性阵发有轻度至中度抑制，持续至第90 - 120分钟。静脉注射剂量为100mg/kg的N - 氨甲基哌嗪3,3 - 二乙基 - 2,4 - 吡啶二酮（DKMP），可使戊四氮阈值（“n”）提高3.5至4倍，N阈值提高8 - 10倍，接近地西泮（静脉注射10mg/kg）的效果。在注射DKMP的情况下难以达到癫痫状态，而在已发生癫痫状态时，50mg/kg剂量的DKMP可完全抑制癫痫发作表现。在已发生青霉素癫痫的情况下注射DKMP可导致全身性阵发活动完全抑制，持续至第100 - 120分钟。
