ANIRACETAM REVERSES THE ANTICONVULSANT ACTION OF NBQX AND GYKI 52466 IN DBA/2 MICE

被引:38
作者
CHAPMAN, AG
ALZUBAIDY, Z
MELDRUM, BS
机构
[1] Department of Neurology, Institute of Psychiatry, De Crespigny Park, Denmark Hill
基金
英国医学研究理事会;
关键词
DBA/2; MICE; ANIRACETAM; AMPA RECEPTOR ANTAGONISTS; NBQX (2,3-DIHYDROXY-6-NITRO-7-SULFAMOYLBENZO(F)QUINOXALINE); GYKI 52466 (1-(4-AMINOPHENYL)-4-METHYL-7,8-METHYLENEDIOXY-5H-2,3-BENZODIAZEPINE.HCL); CPPENE (D(-)-(E)-4-(3-PHOSPHONOPROP-2-ENYL) PIPERAZINE-2-CARBOXYLIC ACID);
D O I
10.1016/0014-2999(93)90465-T
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Aniracetam (1-p-anisoyl-2-pyrrolidinone) selectively reverses the anticonvulsant activities of the non-NMDA receptor antagonists, GYKI 52466 (1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine . HCl) and, to a lesser extent, NBQX (2,3-dihydroxy-6-nitro-7-sulfamoylbenzo(F)quinoxaline), without affecting the anticonvulsant activity of the competitive NMDA receptor antagonist, D(-)-CPPene, in DBA/2 mice. Pretreatment with aniracetam (50 nmol i.c.v., 15 min before drugs) increases the ED50 values (mumol/kg i.p., 15 min) for GYKI 52466-induced protection against sound-induced clonic seizures in DBA/2 mice 7 fold, from 20.1 (11.9-33.9) to 142 (91.7-219), and for NBQX-induced protection 2 fold, from 39.7 (33.8-46.7) to 85.6 (63.9-115), respectively. Aniracetam on its own (12.5-100 nmol i.c.v.) has no convulsant activity, but reverses the anticonvulsant effect of GYKI 52466 (60 mumol/kg i.p., 15 min) in a dose-dependent manner.
引用
收藏
页码:301 / 303
页数:3
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