Ono H, Saito K, Kondo M, Morishita S, Kato K, Hasebe Y, Nakayama M, Kato F, Nakamura T, Satoh M
Department of Toxicology and Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Arzneimittelforschung. 1990 Jul;40(7):730-5.
Effects of KW-6629 (7-chloro-N,N,3-trimethylbenzo[b]furan-2-carboxamide) were studied with special reference to the effect on motor and central nervous systems using rats. The drug effectively reduced the motor coordination (rotarod), the anemic decerebrate rigidity, the crossed extensor reflex, and the gamma-activity indirectly recorded from muscle afferent discharges without showing the direct inhibitory effect on muscle spindles. KW-6629 depressed the polysynaptic and dorsal root reflexes without showing marked effect on the monosynaptic reflex in intact spinal cord rats. KW-6629 produced high-amplitude slow wave in the cerebral cortex in electroencephalogram (EEG). KW-6629 did not reduce the EEG after-discharges and behavioral convulsion (amygdaloid kindling). KW-6629 had no effect on the neuromuscular junction. These results suggest that KW-6629 is a centrally acting muscle relaxant which has a site of action in supraspinal structures.
以大鼠为实验对象,特别参照KW-6629(7-氯-N,N,3-三甲基苯并[b]呋喃-2-甲酰胺)对运动和中枢神经系统的影响进行了研究。该药物有效降低了运动协调性(转棒试验)、贫血性去大脑强直、交叉伸肌反射以及从肌肉传入放电间接记录的γ活动,而对肌梭未表现出直接抑制作用。KW-6629抑制了多突触反射和背根反射,而对完整脊髓大鼠的单突触反射未表现出明显影响。KW-6629在脑电图(EEG)中可在大脑皮层产生高振幅慢波。KW-6629并未减少EEG的后放电和行为性惊厥(杏仁核点燃)。KW-6629对神经肌肉接头无影响。这些结果表明,KW-6629是一种中枢性肌肉松弛剂,其作用位点位于脊髓上结构。