Albertson T E, Joy R M, Stark L G
Epilepsia. 1984 Aug;25(4):511-7. doi: 10.1111/j.1528-1157.1984.tb03453.x.
The anticonvulsant properties of fluzinamide (AHR-8559) were evaluated in the kindled amygdaloid seizure model in rats. Fluzinamide significantly attenuated afterdischarge durations and the severity of the accompanying convulsive responses in previously kindled rats at doses that did not cause sedation or ataxia. After acute intraperitoneal injections, the maximum anticonvulsant effectiveness against suprathreshold (400 microA) stimulation was seen at 30 min. Fluzinamide (10-80 mg/kg i.p.) was also evaluated in previously kindled rats using threshold (20-microA increments) seizures. Low doses of fluzinamide significantly elevated seizure threshold and reduced both elicited afterdischarge durations and seizure severity. When administered daily during kindling acquisition, fluzinamide (20 and 40 mg/kg i.p.) significantly increased the number of trials necessary to complete kindling. The duration and the severity of the responses induced by stimulations during the acquisition period were reduced. Previous studies have shown that the anticonvulsant profile for fluzinamide, as determined by traditional electrical and clinical models of epilepsies, most closely resembled phenobarbital and valproic acid, and differed from phenytoin and ethosuximide. The current study is consistent with this profile, with fluzinamide--like phenobarbital and valproic acid--significantly modifying both acquisition of kindling and the fully kindled amygdaloid seizure.
在大鼠杏仁核点燃癫痫模型中评估了氟齐酰胺（AHR - 8559）的抗惊厥特性。氟齐酰胺在不引起镇静或共济失调的剂量下，能显著缩短先前点燃大鼠的放电后持续时间以及伴随惊厥反应的严重程度。急性腹腔注射后，在30分钟时观察到对阈上（400微安）刺激的最大抗惊厥效果。还使用阈下（20微安递增）癫痫发作对先前点燃的大鼠评估了氟齐酰胺（10 - 80毫克/千克腹腔注射）。低剂量的氟齐酰胺显著提高癫痫发作阈值，并缩短诱发的放电后持续时间和减轻癫痫发作严重程度。在点燃形成过程中每日给药时，氟齐酰胺（20和40毫克/千克腹腔注射）显著增加完成点燃所需的试验次数。在形成期刺激诱发的反应持续时间和严重程度均降低。先前的研究表明，根据传统的癫痫电模型和临床模型确定，氟齐酰胺的抗惊厥谱与苯巴比妥和丙戊酸最为相似，与苯妥英和乙琥胺不同。当前的研究与这一谱型一致，氟齐酰胺与苯巴比妥和丙戊酸一样，能显著改变点燃的形成以及完全点燃的杏仁核癫痫发作。
