Lewin E, Bleck V
Epilepsia. 1985 May-Jun;26(3):258-61. doi: 10.1111/j.1528-1157.1985.tb05415.x.
The effect in mice of inosine administered subcutaneously on the threshold of seizures induced with pentylenetetrazole (PTZ), bicuculline, and picrotoxin was studied, and brain inosine levels were measured. Following inosine, 1,000 mg/kg, the threshold to PTZ was increased at 10-30 min after injection as determined by a tail vein infusion method. Bicuculline and picrotoxin thresholds were significantly elevated only at 5 min. The time to the first myoclonic jerk after intraperitoneal administration of each of these convulsants was significantly prolonged by the lowest dose of inosine tested (250 mg/kg for PTZ, 100 mg/kg for bicuculline, and 500 mg/kg for picrotoxin). Inosine was given subcutaneously 10 min before the convulsant. The mean control brain inosine concentration was 2.9 microM. After subcutaneous inosine, 1,000, 500, and 250 mg/kg, the highest levels reached were 14.4, 7.9, and 4.3 microM, respectively. It is concluded that micromolar concentrations of inosine in brain are antiepileptic.
研究了皮下注射肌苷对小鼠戊四氮（PTZ）、荷包牡丹碱和印防己毒素所致癫痫发作阈值的影响，并测定了脑内肌苷水平。注射1000mg/kg肌苷后，采用尾静脉输注法测定，注射后10 - 30分钟PTZ阈值升高。荷包牡丹碱和印防己毒素阈值仅在5分钟时显著升高。每种惊厥剂腹腔注射后首次肌阵挛抽搐的时间被测试的最低剂量肌苷（PTZ为250mg/kg，荷包牡丹碱为100mg/kg，印防己毒素为500mg/kg）显著延长。在惊厥剂注射前10分钟皮下注射肌苷。脑内肌苷平均对照浓度为2.9微摩尔。皮下注射1000、500和250mg/kg肌苷后，达到的最高水平分别为14.4、7.9和4.3微摩尔。结论是脑内微摩尔浓度的肌苷具有抗癫痫作用。
