Kainic acid derivatives with anticonvulsant activity.
beta-Kainic acid, and the glycine and amino-methylphosphonate derivatives of alpha- and beta-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. ED50 values against clonus are (in mumol): beta-kainic acid, 0.09; beta-kainylglycine, 0.11; alpha-kainylglycine, 0.28; alpha-kainylaminomethylphosphonate, 0.31; beta-kainylaminomethylphosphonate, greater than 1.5. In addition a direct convulsant effect occurs after the alpha-kainyl derivatives.
D000161:Acoustic Stimulation; D000818:Animals; D000927:Anticonvulsants; D004353:Drug Evaluation, Preclinical; D005260:Female; D007608:Kainic Acid / Q000031:analogs & derivatives*; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D011759:Pyrrolidines; D012640:Seizures / Q000517:prevention & control
D000927:Anticonvulsants; D011759:Pyrrolidines; D007608:Kainic Acid