Büch H P, Baldauf J, Wolff I
Arzneimittelforschung. 1980;30(12):2117-23.
3 min after simultaneous i.v. administration of phenazone (200 mg/kg) and of pentetrazole (50 mg/kg) or of phenazone and of the convulsively active S-(+)-1-methyl-5-phenyl-5-propyl barbituric acid = (+)-MPPB (75 mg/kg), respectively, phenazone concentrations in liver, spleen and fat tissue of rats are lower, in brain tissue, however, it is higher than those of the control (rats receiving phenazone only); the distribution pattern of (+)-MPPB between the tissues corresponds to that of phenazone after simultaneous administration of pentetrazole. In rats anaesthetized by hexobarbital (35 mg/kg) or by the anaesthetically active R-(-)- 1-methyl-5-phenyl-5-propyl barbituric acid = (-)-MPPB (75 mg/kg), respectively, phenazone tissue distribution is at the same time (3 min) not different from that of the control; the tissue distribution pattern of (-)-MPPB corresponds to that of phenazone after simultaneous administration of hexobarbital. Following pretreatment with diazepam, reserpine and phenoxybenzamine, respectively, the tissue distribution pattern of (+)-MPPB, in the rats approaches that of (-)-MPPB. The distribution of (-)-MPPB in the tissues corresponds to that of (+)-MPPB, if the animals receive simultaneously pentetrazole or are electrically stimulated, respectively, to cause a convulsive seizure.
分别同时静脉注射非那宗(200毫克/千克)和戊四氮(50毫克/千克)或非那宗和惊厥活性的S-(+)-1-甲基-5-苯基-5-丙基巴比妥酸= (+)-MPPB(75毫克/千克)3分钟后,大鼠肝脏、脾脏和脂肪组织中的非那宗浓度较低,然而在脑组织中,其浓度高于对照组(仅接受非那宗的大鼠);同时注射戊四氮后,(+)-MPPB在各组织间的分布模式与非那宗的分布模式一致。分别用己巴比妥(35毫克/千克)或麻醉活性的R-(-)-1-甲基-5-苯基-5-丙基巴比妥酸= (-)-MPPB(75毫克/千克)麻醉大鼠后,同一时间(3分钟)非那宗的组织分布与对照组无异;同时注射己巴比妥后,(-)-MPPB的组织分布模式与非那宗的分布模式一致。分别用安定、利血平和酚苄明预处理后,大鼠体内(+)-MPPB的组织分布模式接近(-)-MPPB的分布模式。如果动物分别同时接受戊四氮或接受电刺激以引发惊厥发作,(-)-MPPB在组织中的分布与(+)-MPPB的分布一致。