KAINIC ACID-DERIVATIVES WITH ANTICONVULSANT ACTIVITY

被引:31
作者
COLLINS, JF
DIXON, AJ
BADMAN, G
DESARRO, G
CHAPMAN, AG
HART, GP
MELDRUM, BS
机构
[1] INST PSYCHIAT, DEPT NEUROL, LONDON SE5 8AF, ENGLAND
[2] SIR JOHN CASS SCH SCI & TECHNOL, DEPT CHEM, 31 JEWRY ST, LONDON EC3N 2EY, ENGLAND
关键词
D O I
10.1016/0304-3940(84)90405-1
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
.beta.-Kainic acid, and the glycine and amino-methylphosphonate derivatives of .alpha.- and .beta.-kainic acid, were injected intracerebroventricularly in DBA/2 mice, that show sound-induced seizure responses. An anticonvulsant effect is observed with marked protection against the tonic and clonic phases of the seizure response. ED50 values against clonus are (in .mu.mol); .beta.-kainic acid, 0.09; .beta.-kainylglycine, 0.11; .alpha.-kainylglycine, 0.28; .alpha.-kainylaminomethylphosphonate, 0.31; .beta.-kainylaminomethylphosphonate, > 1.5. A direct convulsant effect occurs after the .alpha.-kainyl derivatives.
引用
收藏
页码:371 / 376
页数:6
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