β-咔啉ZK 91296在大鼠遗传性失神癫痫模型中的抗癫痫作用

Antiepileptic action of the beta-carboline ZK 91296 in a genetic petit mal model in rats.

作者信息

Jensen L H, Marescaux C, Vergnes M, Micheletti G, Petersen E N

出版信息

Eur J Pharmacol. 1984 Jul 20;102(3-4):521-4. doi: 10.1016/0014-2999(84)90574-0.

Abstract

The anticonvulsant action of the benzodiazepine (BZ) receptor partial agonist, ethyl 5-benzyloxy-4-methoxymethyl-beta-carboline-3-carboxylate (ZK 91296) was studied in rats of Wistar origin exhibiting spontaneous bilateral cortical synchronous spike and wave discharges with a symptomatology paralleling that of human petit mal seizures. ZK 91296 1-16 mg/kg i.p.) attenuated the absence seizures without inducing signs of sedation or disorganized EEG patterns at any dose. Diazepam (1-8 mg/kg i.p.) suppressed seizures but also induced sedation and modified EEG background activity in a dose-related manner.

摘要

在起源于Wistar的大鼠中研究了苯二氮䓬（BZ）受体部分激动剂5-苄氧基-4-甲氧基甲基-β-咔啉-3-羧酸乙酯（ZK 91296）的抗惊厥作用，这些大鼠表现出自发性双侧皮质同步棘波和慢波放电，其症状与人类失神发作相似。腹腔注射ZK 91296（1-16毫克/千克）可减轻失神发作，且在任何剂量下均未引起镇静迹象或脑电图模式紊乱。地西泮（腹腔注射1-8毫克/千克）可抑制癫痫发作，但也会引起镇静，并以剂量相关的方式改变脑电图背景活动。