[Anti-epileptic effect of the new calcium channel blocker IOS-1.1212].
In experiments on freely moving male Wistar rats it was shown that IOS-1.1212 (1,4-dihydropyridine) in a dose 2 and 10 mg/kg (i. p.) suppressed the penicillin-induced focal epileptic activity in cerebral cortex. Similar suppressing effect of IOS-1.1212 was shown on acute generalized tonic-clonic pentylenetetrazol (PTZ) seizures (75 mg/kg i. p.) and on chronic PTZ administration (PTZ-kindling, 30 mg/kg i. p. during 30 days): when injected 30 min before each PTZ administration it delayed the development of kindling-induced seizures susceptibility in randomized animals (series 1) and attenuated the severity of seizures in PTZ-sensitive animals (series 2). However, IOS-1.1212 had no effect on the strychnine-induced focal epileptic activity. In male Icr:Icl mice IOS-1.1212 in a dose 1.5 and 5 mg/kg also influenced the PTZ convulsions (i. v. titration of 1% solution at a rate of 0.01 ml/s) and had no effect on the strychnine convulsions (i. v. titration of 0.01% solution at a rate of 0.01 ml/s) and on maximal electroshock. In addition, IOS-1.1212 significantly increased antiepileptic effect of phenobarbital on maximal electroshock.
Karpova
M N
MN
Pankov
O Iu
OIu
Glebov
R N
RN
Dubur
G Ia
GIa
Germane
S K
SK
Klusha
V E
VE
D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology* / Q000627:therapeutic use; D002121:Calcium Channel Blockers / Q000494:pharmacology* / Q000627:therapeutic use; D004095:Dihydropyridines / Q000378:metabolism / Q000494:pharmacology*; D004827:Epilepsy / Q000139:chemically induced / Q000188:drug therapy*; D008297:Male; D010406:Penicillins / Q000633:toxicity; D010433:Pentylenetetrazole / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains; D013331:Strychnine / Q000633:toxicity
D000927:Anticonvulsants; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D010406:Penicillins; C073838:2,6-dimethyl-3,5-bis(2'-propoxyethoxycarbonyl)-4-(2''-difluoromethoxyphenyl)-1,4-dihydropyridine; C038806:1,4-dihydropyridine; D013331:Strychnine; D010433:Pentylenetetrazole
Antiépilepticheskie éffekty novogo blokatora Ca-kanalov IOS-1.1212.