[The anticonvulsant properties of glutapyrone--a new type of derivative of amino acid-containing 1,4-dihydropyridines].
Experiments on male Wistar rats and Icr:Icl mice studied the influence of the novel compound--amino acid-containing 1,4-dihydropyridine derivative glutapyrone (G) on acute generalized seizures, arecoline and nicotine tremor, and 45Ca2+ uptake in brain synaptosomes. It was shown that G produced significant antiepileptic effects on models of acute pentylenetetrazole seizures on rats and mice. Efficiency of antiepileptic effect depended on a dose and method of modeling seizures: it was more effective in case of intravenously pentylenetetrazole-induced seizure tested by clonic and tonic seizure components and death. The results suggest the participation of GABAergic system in realization of antiepileptic effect of G. Glutapyrone did not influence the 45Ca2+ uptake by rat cortical synaptosomes (evoked by a 1-min depdariration with 55 mM K+), this suggests that G lacked calcium antagonist properties characteristic of 1,4-dihydropyridine compounds such as nifedipine, nimodipine. In addition, G does not affect N- and M-cholinergic processes.
Karpova
M N
MN
Germane
S K
SK
Cebers
G
G
Pankov
O Iu
OIu
Klusa
V E
VE
Duburs
G Ia
GIa
Bisenieks
E A
EA
D000818:Animals; D000927:Anticonvulsants / Q000627:therapeutic use*; D001115:Arecoline; D002118:Calcium / Q000378:metabolism; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D004095:Dihydropyridines / Q000627:therapeutic use*; D004353:Drug Evaluation, Preclinical; D004829:Epilepsy, Generalized / Q000139:chemically induced / Q000188:drug therapy / Q000378:metabolism; D005971:Glutamates / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009538:Nicotine; D010433:Pentylenetetrazole; D051381:Rats; D017208:Rats, Wistar; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism; D014202:Tremor / Q000139:chemically induced / Q000188:drug therapy / Q000378:metabolism
D000927:Anticonvulsants; D004095:Dihydropyridines; D005971:Glutamates; C086069:glutapyrone; D001115:Arecoline; D009538:Nicotine; D002118:Calcium; D010433:Pentylenetetrazole
Protivosudorozhnye svoĭstva glutapirona--proizvodnogo novogo tipa--aminokislot-soderzhashchikh 1,4-digidropiridinov.