INHIBITION OF AMINOPHYLLINE-INDUCED CONVULSIONS IN MICE BY ANTIEPILEPTIC DRUGS AND OTHER AGENTS
INHIBITION OF AMINOPHYLLINE-INDUCED CONVULSIONS IN MICE BY ANTIEPILEPTIC DRUGS AND OTHER AGENTS
复制标题
DOI：
10.1016/0014-2999(87)90383-9
复制
发表时间：
1987-12-15
影响因子：
5
通讯作者：
KLEINROK, Z
中科院分区：
文献类型：
--
作者：
CZUCZWAR, SJ;JANUSZ, W;KLEINROK, Z
研究了常见的抗癫痫药物和影响不同神经递质系统的药物对氨茶碱（280 mg/kg i.p.）引起的小鼠惊厥的影响。所有药物和药剂均经腹膜内施用。地西泮和苯巴比妥拮抗整个癫痫发作模式，阵挛期的 ED50 值分别为 3.5 和 62 mg/kg。 500 mg/kg 的丙戊酸可以保护不到 50% 的小鼠免受阵挛期的影响。其余抗癫痫药（乙酰唑胺，最高 1000 mg/kg；卡马西平和二苯内酰脲，最高 50 mg/kg；乙舒酰亚胺，500 mg/kg 和三甲二酮，400 mg/kg）在这方面完全无效。普萘洛尔（高达20mg/kg）、巴氯芬（20mg/kg）、γ-羟基丁酸（300mg/kg）、氨氧乙酸（20mg/kg）、可乐定（高达0.2mg/kg）、氯胺酮（30mg/kg）、阿托品（20mg/kg）、罂粟碱（50mg/kg）和L-苯基异丙基腺苷(2 mg/kg)也不影响阵挛期。只有N-甲基-D-天冬氨酸兴奋拮抗剂、2-氨基-5-膦酰基戊酸和2-氨基-7-膦酰基庚酸才能提供针对氨茶碱诱导的阵挛性癫痫发作活动的保护。结果表明，氨茶碱惊厥对抗癫痫药物相对耐药，表明兴奋性传递拮抗剂是潜在的抗氨茶碱药物。
Common antiepileptic drugs and agents affecting different neurotransmitter systems were studied against aminophylline (280 mg/kg i.p.)-induced convulsions in mice. All drugs and agents were administered i.p. Diazepam and phenobarbital antagonized the whole seizure pattern and the respective ED50 values for the clonic phase were 3.5 and 62 mg/kg. Valproate at 500 mg/kg protected fewer than 50% of mice against the clonic phase. The remaining antiepileptics (acetazolamide, up to 1000 mg/kg; carbamazepine and diphenylhydantoin, up to 50 mg/kg; ethosuximide, 500 mg/kg and trimethadione, 400 mg/kg) were totally ineffective in this respect. Propranolol (up to 20 mg/kg), baclofen (20 mg/kg), .gamma.-hydroxybutyric acid (300 mg/kg), aminooxyacetic acid (20 mg/kg), clonidine (up to 0.2 mg/kg), ketamine (30 mg/kg), atropine (20 mg/kg), papaverine (50 mg/kg) and L-phenylisopropyladenosine (2 mg/kg) did not affect the clonic phase either. Only antagonists of N-methyl-D-aspartic acid excitation, 2-amino-5-phosphonopentanoic acid and 2-amino-7-phosphonoheptanoic acid afforded protection against aminophylline-induced clonic seizure activity. The results show that aminophylline convulsions are relatively resistant to antiepileptic drugs and suggest that antagonists of excitatory transmission are potential antiaminophylline drugs.