Preliminary evaluation of anticonvulsant activity and neurotoxicity of some 1,4-substituted piperazine derivatives.
A series of 1,4-piperazine derivatives was synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (ScMet) assays and for neurotoxicity (TOX). The compounds were only moderately effective. The anticonvulsant activity was accompanied by neurotoxicity. 1-[(4-Chlor-3-methylphenoxy)-acetyl]-4-(2-methoxyphenyl)-piperazine was also evaluated in six hertz seizure test (6-Hz) and showed good activity. At the dose of 100 mg/kg b. w. the compound produced 100% protection after 0.5 h without neurotoxic effect.
Marona
Henryk
H
Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna St., 30-688 Kraków, Poland. hen.mar@interia.pl
Gunia
Agnieszka
A
Słoczyńska
Karolina
K
Rapacz
Anna
A
Filipek
Barbara
B
Cegła
Marek
M
Opoka
Włodzimierz
W
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D004195:Disease Models, Animal; D004597:Electroshock; D008297:Male; D051379:Mice; D020258:Neurotoxicity Syndromes / Q000209:etiology*; D010433:Pentylenetetrazole; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D012640:Seizures / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D010879:Piperazines; D010433:Pentylenetetrazole