General pharmacology of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole difumarate. 1st communication: effects on the central nervous system.
Effects of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole difumarate (KB-2413) on the central nervous system were compared with those of ketotifen and chlorpheniramine. Among the various activities related to the central nervous system, KB-2413 showed inhibitory effects on locomotor activity, acetic acid-induced writhing in mice and reserpine-induced hypothermia in rats at a high dose such as 100 mg/kg p.o. However, in mice, it (10-100 mg/kg p.o.) exerted no significant influence on muscle tone, various experimental convulsions, oxotremorine-induced tremor, physostigmine-induced mortality or hexobarbital-induced sleep, and in rats, it had no effect on rectal temperature or conditioned avoidance. It also did not affect spontaneous electroencephalogram (EEG), EEG arousal responses or photic driving response in rabbits at 5 mg/kg i.v. On the other hand, ketotifen and chlorpheniramine affected more widely and strongly the central nervous system than KB-2413. In conclusion, KB-2413 showed a less potent effect on the central nervous system than ketotifen and chlorpheniramine, and no results suggested serious side effects of KB-2413.
D000085:Acetates / Q000037:antagonists & inhibitors; D000374:Aggression / Q000187:drug effects; D000818:Animals; D000927:Anticonvulsants; D001562:Benzimidazoles / Q000494:pharmacology*; D001831:Body Temperature / Q000187:drug effects; D001921:Brain / Q000187:drug effects*; D006168:Guinea Pigs; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009125:Muscle Relaxants, Central; D010095:Oxotremorine / Q000037:antagonists & inhibitors; D010830:Physostigmine / Q000037:antagonists & inhibitors / Q000633:toxicity; D004856:Postural Balance / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D012890:Sleep / Q000187:drug effects
D000085:Acetates; D000927:Anticonvulsants; D001562:Benzimidazoles; D006635:Histamine H2 Antagonists; D009125:Muscle Relaxants, Central; D010095:Oxotremorine; C043345:emedastine; D010830:Physostigmine