Kainic acid derivatives with anticonvulsant activity

Abstract β-Kainic acid, and the glycine and amino-methylphosphonate derivatives of α- and β-kainic acid, have been 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. ED 50 values against clonus are (in μmol): β-kainic acid, 0.09; β-kainylglycine, 0.11; α-kainylglycine, 0.28; α-kainylaminomethylphosphonate, 0.31; β-kainylaminomethylphosphonate, >1.5. In addition a direct convulsant effect occurs after the α-kainyl derivatives.