Comparative study of the anticonvulsive activity of N-aminomethylpiperazine-3,3-diethyl 2,4-pyridinedione with the activity of known antiepileptic agents.
N-aminomethylpiperazine-3,3-diethyl-2,4-pyridinedione (DKMP) is a newly synthesized compound with a marked anticonvulsive effect in various epileptic models. The aim of the present work is to compare its anticonvulsive effect in corazol convulsions (100 mg/kg corazol, s.c.) with known anticonvulsants applied in clinical practice. The compounds tested were applied subcutaneously in equitoxic doses (1/20 and 1/30 of their respective LD50). Some undesirable side effects of the antiepileptic agents tested were also studied. With the experimental model used, DKMP was found to have a better anticonvulsive effect compared with diphenylhydantoin, depakin, suxilep and phenobarbital. Diazepam completely inhibited the convulsions, but it has an undesirable strong myorelaxing effect. In a subchronical experiment it was found that no tolerance developed toward DKMP, while the anticonvulsant effect of diazepam significantly decreased on the 15th day, compared with a single administration. Using the rota-rod test it was found that the agents studied had a stronger neurotoxic action compared with DKMP. These results outline DKMP as a promising compound with good antiepileptic activity, comparable to that of the known anticonvulsants.
D000818:Animals; D000927:Anticonvulsants / Q000627:therapeutic use* / Q000633:toxicity; D004353:Drug Evaluation, Preclinical; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009043:Motor Activity / Q000187:drug effects; D010433:Pentylenetetrazole / Q000494:pharmacology; D011728:Pyridones / Q000627:therapeutic use* / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy
D000927:Anticonvulsants; D011728:Pyridones; C033227:N-aminomethylpiperazine 3,3-diethyl-2,4-pyridinedione; D010433:Pentylenetetrazole