ANTICONVULSANT ACTIVITY OF PYRROLO[1',2'-1,2]IMIDAZO[4,5-B]PYRIDINES,PYRROLO[2',1'-2,3]IMIDAZO[4,5-C] PYRIDINES AND PYRROLO[2,1-F]PURINES IN DBA 2 MICE/
A. Desarro et al., ANTICONVULSANT ACTIVITY OF PYRROLO[1',2'-1,2]IMIDAZO[4,5-B]PYRIDINES,PYRROLO[2',1'-2,3]IMIDAZO[4,5-C] PYRIDINES AND PYRROLO[2,1-F]PURINES IN DBA 2 MICE/, General pharmacology, 25(5), 1994, pp. 1027-1031
1. The behavioural and anticonvulsant effects of eight pyrrolimidazopy
ridines (PI(1)a-d and PI(2)a-d) and four pyrrolopurines (PP) were stud
ied after intraperitoneal administration in DBA/2 mice, a strain genet
ically susceptible to sound-induced seizures. 2. The anticonvulsant ef
fects were evaluated in DBA/2 mice on seizures evoked by means of audi
tory stimulation (109 dB, 12-16 kHz) in animals placed singly under a
perspex dome. 3. Hypothermic activity was observed after the highest d
oses of the pyrroloderivatives studied. 4. Our study demonstrated that
the anticonvulsant effect of pyrroloimidazopyridines H-pyrrolo-[1',2'
:1,2]imidazo[4,5-b]pyridin-6-ones) and pyrrolopurines (PP) was general
ly better than corresponding pyrrolobenzimidazoles (PB) and pyrroloimi
dazopyridines 8H-pyrrolo[2',1':2,3]imidazo[4,5-c]pyridin-8-ones) and,
in some cases, comparable to that of phenytoin and desmethylclobazam.
5. The anticonvulsant potency of the derivatives studied cannot be dir
ectly related to their lipophilicity.