Anticonvulsant properties of two new 3,3-diethyl-2,4-pyridinedione derivatives. I. Effects in two experimental models of generalized epilepsy in cats.
The anticonvulsant properties of two N-aminomethyl derivatives of 3,3-diethyl-2,4-pyridinedione (persedon) are studied on two experimental models of generalized (pentylenetetrazol and penicillin) epilepsy in cats. N-aminomethylmorpholine 3,3-diethyl-2,4-pyridinedione (DKMM) applied in doses of 100 mg/ng i. v. in cases of pentylenetetrazol epilepsy leads to a rise in the convulsive thresholds (n, N) by 1.5 and two times, respectively. Administration of the drug in the same dose on developed penicillin epilepsy in cats reveals slight to moderate suppression of the generalized paroxysms, lasting until the 90th-120th min. N-aminomethylpiperazine 3,3-diethyl-2,4-pyridinedione (DKMP), injected in a dose of 100 mg/kg i. v., raises the pentylenetetrazol threshold ("n") 3.5 to 4 times and 8-10 times the N-threshold, approaching the effect of diazepam (10 mg/kg i. v.). On the background of injected DKMP it is difficult to attain epileptic status, and in the case of developed epileptic status DKMP in a dose of 50 mg/kg suppresses completely the seizure manifestations. Injection of DKMP in the cases of developed penicillin epilepsy results in complete suppression of the generalized paroxysmal activity, lasting until the 100th-120th min.
D000818:Animals; D000927:Anticonvulsants / Q000627:therapeutic use*; D001921:Brain / Q000187:drug effects / Q000503:physiopathology*; D002415:Cats; D004195:Disease Models, Animal; D010433:Pentylenetetrazole; D011728:Pyridones / Q000627:therapeutic use*; D012640:Seizures / Q000188:drug therapy*
D000927:Anticonvulsants; D011728:Pyridones; C033226:N-aminomethylmorpholine 3,3-diethyl-2,4-pyridinedione; C033227:N-aminomethylpiperazine 3,3-diethyl-2,4-pyridinedione; D010433:Pentylenetetrazole