[Combined blockade of AMPA- and NMDA-receptors has maximum effect to eliminate development of pentylenetetrazole-induced kindling in rats].
Peroral chronic administration the standard antiepileptic drug sodium valproate in a dose of 200 mg/kg eliminates development of generalized clonic-tonic pentylenetetrazol kindling seizures in 100% of rats, but only in 57% of rats this treatment prevents clonic kindling seizures. In the specified dose sodium valproate decreases in 1.7 times average severity of pentylenetetrazol kindling seizures compare with control. IEM-2121, causing combined blockade of NMDA- and AMPA-glutamate receptors, as well as IEM-1676, which also blocks AMPA-, NMDA- and N-cholinoreceptors, both after peroral chronic administration in a doses 10 mg/kg and 20 mg/kg accordingly, possess higher, than sodium valproate, anticonvulsant activity because reduce average severity of pentylenetetrazol kindling seizures in 2.4-2.7 times in comparison with control and prevents clonic kindling seizures in 87% of rats. Combined blockade of AMPA- and NMDA-receptors and perhars N-cholinoreceptors has maximum effect to eliminate epileptogenesis both clonic, and clonic-tonic pentylenetetrazol kindling seizures.
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Veselkina
D000218:Adamantane / Q000031:analogs & derivatives* / Q000494:pharmacology*; D000284:Administration, Oral; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D004334:Drug Administration Schedule; D008297:Male; D010433:Pentylenetetrazole; D051381:Rats; D017208:Rats, Wistar; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D011950:Receptors, Cholinergic / Q000378:metabolism; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology; D012720:Severity of Illness Index; D014635:Valproic Acid / Q000494:pharmacology
D000927:Anticonvulsants; D018091:Receptors, AMPA; D011950:Receptors, Cholinergic; D016194:Receptors, N-Methyl-D-Aspartate; D014635:Valproic Acid; D000218:Adamantane; D010433:Pentylenetetrazole