非氨酯及其他化合物对N-甲基-D-天冬氨酸诱导的小鼠惊厥和致死率的比较作用。

Comparative effects of felbamate and other compounds on N-methyl-D-aspartic acid-induced convulsions and lethality in mice.

作者信息

Sofia R D, Gordon R, Gels M, Diamantis W

机构信息

Wallace Laboratory, Division of Carter-Wallace, Inc., Cranbury, New Jersey 08512.

出版信息

Pharmacol Res. 1994 Feb-Mar;29(2):139-44. doi: 10.1016/1043-6618(94)80037-5.

DOI:10.1016/1043-6618(94)80037-5

PMID:8058587

Abstract

Felbamate and selected compounds were evaluated for their ability to protect against N-methyl-D-aspartic acid (NMDA)-induced convulsions and lethality in mice. Convulsions produced by intracerebroventricular administration of NMDA (0.8 micrograms per mouse) were antagonized by felbamate, phenytoin, carbamazepine, phenobarbital, valproate, diazepam, 2-amino-5-phosphonovalergic acid (APV), dextromethorphan and ketamine. NMDA (350 mg kg-1 intraperitoneally) produced 100% lethality in mice. Felbamate, phenytoin, and phenobarbital were ineffective in preventing NMDA-induced lethalities, whereas diazepam, APV, ketamine and dextromethorphan were the most potent compounds in preventing lethalities. Any relationship between the protective effects of felbamate against NMDA-induced seizures and competitive or non-competitive antagonism of NMDA receptor sites, however, cannot be established until further experimentation is carried out.

摘要

对非氨酯及选定的化合物进行了评估，以确定它们在小鼠中预防N-甲基-D-天冬氨酸（NMDA）诱导的惊厥和致死作用的能力。脑室内注射NMDA（每只小鼠0.8微克）所产生的惊厥受到非氨酯、苯妥英、卡马西平、苯巴比妥、丙戊酸盐、地西泮、2-氨基-5-磷酸基戊酸（APV）、右美沙芬和氯胺酮的拮抗。NMDA（腹腔注射350毫克/千克）在小鼠中产生100%的致死率。非氨酯、苯妥英和苯巴比妥在预防NMDA诱导的致死作用方面无效，而地西泮、APV、氯胺酮和右美沙芬是预防致死作用最有效的化合物。然而，在进行进一步实验之前，无法确定非氨酯对NMDA诱导的癫痫发作的保护作用与NMDA受体位点的竞争性或非竞争性拮抗之间的任何关系。