Anticonvulsant activity of the imidazoline 6,7-benzoidazoxan.
The effects of the imidazoline 6,7-benzoidazoxan on seizure threshold were assessed using standard tests of anticonvulsant activity. Benzoidazoxan (10-30 mg/kg i.p.; 100 mg/kg p.o.) prevented tonic, but not clonic, convulsions induced by electroshock in mice. The increase in seizure threshold was of rapid onset, and, although of short duration, was comparable with that obtained using phenytoin and sodium valproate. Moreover, unlike sodium valproate, benzoidazoxan was an efficacious anticonvulsant at doses (20, 30 mg/kg i.p.) which did not impair rotarod performance. The anticonvulsant effects of benzoidazoxan were confirmed using the maximal electroshock test in mice (median effective dose, 13.2 mg/kg i.p.) and rats (anticonvulsant at 30 mg/kg i.p.). In addition, benzoidazoxan (10, 30 mg/kg i.p.) prevented tonic, but not clonic, seizures induced by bicuculline in mice. Thus, the imidazoline benzoidazoxan was found to be a novel anticonvulsant agent against electrically and chemically induced seizures in mice and rats with a profile of action similar to that of phenytoin.
Jackson
H C
HC
Reckitt & Colman Psychopharmacology Unit, Department of Pharmacology, School of Medical Sciences, Bristol, U.K.
Ripley
T L
TL
Dickinson
S L
SL
Nutt
D J
DJ
D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D001640:Bicuculline; D004146:Dioxanes / Q000494:pharmacology*; D004597:Electroshock; D007093:Imidazoles / Q000494:pharmacology*; D008297:Male; D051379:Mice; D010672:Phenytoin / Q000494:pharmacology; D004856:Postural Balance / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D014635:Valproic Acid / Q000494:pharmacology
D000927:Anticonvulsants; D004146:Dioxanes; D007093:Imidazoles; C073312:6,7-benzoidazoxan; D014635:Valproic Acid; D010672:Phenytoin; D001640:Bicuculline