Pharmacological study on 5-(o-chlorophenyl)-1- methyl-7-nitro-1, 3-dihydro-2H-1, 4-benzodiazepin-2-one (ID-690) with special reference to the effects on motor systems

Abstract

Effects of ID-690 on motor systems were compared with those of clonazepam, diazepam and nitrazepam. ID-690 exerted muscle relaxant action in the rotarod method using rats and mice; this action was almost equal in potency to clonazepam and nitrazepam and more potent than diazepam. Pretreatment with ID-690, clonazepam and nitrazepam increased the sleeping time of mice under thiopental anesthesia to the same degree, whereas diazepam produced a lesser effect. ID-690 was almost equal in potency to diazepam and nitrazepam in protecting against oxotremorine-induced tremor in mice, and approximately 10 times as potent as clonazepam. The anticonvulsant action of ID-690 was similar to that of clonazepam. These benzodiazepines effectively augmented the dorsal root reflexes, while showing no effects on the ventral root reflexes. Rigidity in rats due to anemic decerebration was not affected after intraduodenal administration of these drugs, while phasic augmentation of the rigidity by mechanical stimulation of the hind limb was clearly depressed. These drugs had no effects on the neuromuscular junction. From these results, it is concluded that ID-690 has a wider pharmacological spectrum than clonazepam, is almost equal in potency to nitrazepam and is more potent than diazepam. © 1977, The Japanese Pharmacological Society. All rights reserved.